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Ring sulfur in the bicyclo ring system

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514277000 - Hetero ring is six-membered consisting of one nitrogen and five carbon atoms

514279000 - Polycyclo ring system having the six-membered hetero ring as one of the cyclos

514299000 - Bicyclo ring system having the six-membered hetero ring as one of the cyclos

514300000 - Plural hetero atoms in the bicyclo ring system

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Entries
DocumentTitleDate
20100004279SOLID MEDICINAL PREPARATION CONTAINING MANNITOL OR LACTOSE - A solid medicinal preparation which contains: (A) a compound of the following formula (I) or a pharmacologically acceptable salt thereof; and (B) mannitol or lactose which, under specific conditions, has a particle size distribution in which the 90% cumulative diameter is 80 to 300 μm. The compound of the formula (I) has the following formula:01-07-2010
20130030014N-(IMIDAZOLIDIN-2-YLIDENE)-HETEROCYCLOPENTA[b]PYRIDINE DERIVATIVES AS MODULATORS OF ALPHA 2 ADRENERGIC RECEPTORS - The present invention relates to novel N-(imidazolidin-2-ylidene)-heterocyclopenta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.01-31-2013
20130085155THIAZOLOPYRIDINE SIRTUIN MODULATING COMPOUNDS - Provided herein are novel sirtuin-modulating compounds of Structural Formula (Ia) and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.04-04-2013
20130085154CRYSTALLINE FORMS OF PRASUGREL SALTS - Salts of prasugrel were prepared including, for example, crystalline forms of prasugrel hydrobromide. These salts are useful, for example, in medicaments that inhibit the aggregation of platelets.04-04-2013
20130035356CRYSTAL OF DIAMINE DERIVATIVE AND METHOD OF PRODUCING SAME - An object of the present invention is to provide a novel crystal form of a compound that has an inhibitory effect on activated blood coagulation factor X and is useful as a pharmaceutical compound for prevention and/or treatment of thrombotic and/or embolic diseases. The present invention provides a novel crystal form of N02-07-2013
20130035355PRASUGREL IN MICRONIZED, CRYSTALLINE FORM AND PHARMACEUTICAL COMPOSITION THEREOF - The present invention relates to Prasugrel or a pharmaceutically acceptable salt thereof, compositions containing said active ingredient as well as pharmaceutical compositions containing said active ingredient or a composition containing said active ingredient. The present invention further relates to methods for the preparation of the novel compositions.02-07-2013
20100041695Thieno[2,3-b]pyridines as Potassium Channel Inhibitors - The invention provides compounds of the formula:02-18-2010
20090156632DOSAGE REGIMEN FOR PRASUGREL - A dosage regimen for treating vascular disease in a human comprising the steps of administering a loading dosage of about 30 mg to 70 mg of loading dose of prasugrel or a pharmaceutically acceptable salt thereof, and thereafter administering a daily dosage regimen of about 7.5 mg to 15 mg maintenance dose of prasugrel or a pharmaceutically acceptable salt thereof.06-18-2009
20090156633Heterocyclic quinolone derivatives that inhbit prolyl hydroxylase activity - Compounds of Formula I are useful inhibitors of HIF prolyl hydroxylases. Compounds of Formula I have the following structure:06-18-2009
20100105722Substituted 4,5,6,7-tetrahydrothienopyridines as KCNQ2/3 Modulators - Substituted tetrahydrothienopyridines corresponding to formula (1)04-29-2010
20100093786PHARMACEUTICAL COMPOSITION CONTAINING LOW-SUBSTITUTED HYDROXYPROPYL CELLULOSE - Disclosed is a pharmaceutical composition containing a compound represented by the general formula (I) below or a pharmacologically acceptable salt thereof, while having improved dissolvability. Specifically disclosed is a pharmaceutical composition containing (A) a compound represented by the general formula (I) below or a pharmacologically acceptable salt thereof, and (B) a low-substituted hydroxypropyl cellulose.04-15-2010
2009004292911-Beta-Hydroxysteroid Dehydrogenase Inhibitors - There is provided a compound having Formula (I) R02-12-2009
20090203730BICYCLIC PPAT INHIBITORS AS ANTIBACTERIAL AGENTS - Disclosed are compounds of Formula I, pharmaceutical compositions comprising Formula I and methods of treating bacterial infections. The disclosed compounds are inhibitors of PPAT (phosphopantetheine adenyl transferase), and are useful in the treatment and prevention of diseases caused by bacteria, particularly bacteria dependent on PPAT, for example, species such 08-13-2009
20130072520ANTIBACTERIAL AGENTS - Compounds of formula (I) have antibacterial activity:03-21-2013
20130072521THIENOPYRIDINE ESTER DERIVATIVE CONTAINING CYANO GROUP, PREPARATION METHOD, USE AND COMPOSITION THEREOF - A compound with the structure of the formula (I) or a pharmaceutically acceptable salt, a preparation method and use thereof are disclosed in the present invention, wherein R is cyano group. The compound provided by the present invention has an antiplatelet aggregation activity and can be used in preparing a medicament for preventing or treating cardiac and cerebral vascular diseases such as coronary artery syndromes, myocardial infarction and myocardial ischemia which are caused by platelet aggregation.03-21-2013
20080306107Compounds - The present invention relates to new compounds of formula (I) wherein R12-11-2008
20090281137INDOL-2-ONE DERIVATIVES FOR THE TREATMENT OF CENTRAL NERVOUS DISORDERS, GASTROINTESTINAL DISORDERS AND CARDIOVASCULAR DISORDERS - The present invention is related to new 3,3-disubstituted indol-2-one derivatives of the general Formula (I)11-12-2009
200902704472-Aryl-and 2-Heteroarylthiazolyl Compounds, Methods for Their Preparation and Use Thereof - The present invention discloses fused heterobicyclic 2-aryl- and 2-heteroarylthiazolyl compounds and their pharmaceutically acceptable salts and esters thereof, which are useful for inhibiting the growth of cancerous cells, inhibiting human breast carcinoma tumor growth in particular and to treat diseases or disorders associated with securin.10-29-2009
20090270446DIAMINE DERIVATIVES - The present invention relates to diamine compounds which inhibit activated blood coagulation factor X and exhibit an anticoagulant effect and there uses for treating various diseases based on thromboembolism.10-29-2009
20090270445Thiazole compounds and methods of use - The invention relates to methods of using thiazole compounds of Formula I and Formula II and compositions thereof for treating diseases mediated by protein kinase B (PKB) such as cancer and other proliferative disorders where the variables have the definitions provided herein.10-29-2009
20110021558THIENO-PYRIDINE DERIVATIVES AS MEK INHIBITORS - A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.01-27-2011
20110021557Deuterium-enriched pyridinonecarboxamides and derivatives - The present invention relates to deuterium-enriched pyridinone carboxamides and their derivatives of the formula I, and pharmaceutically acceptable salts thereof,01-27-2011
20090012115USE OF TP MODULATORS FOR THE TREATMENT OF CARDIOVASCULAR DISORDERS IN ASPIRIN SENSITIVE AND OTHER POPULATIONS - The present invention provides methods and compositions useful in the treatment or prevention of cardiovascular disorders in individuals for whom therapy with a COX-1 enzyme inhibitor is not feasible due to sensitivity, intolerance, or resistance to the inhibitor. Additionally, the invention provides methods of treating cardiovascular disorders in an individual who is receiving a therapeutically effective dose of a TP modulator and is instructed or advised to avoid and/or not to take aspirin or another COX-1 inhibitor.01-08-2009
20080319004DEUTERIUM-ENRICHED CLOPIDOGREL - The present application describes deuterium-enriched clopidogrel, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.12-25-2008
20080293762Preventive and Therapeutic medicament for gastroesophageal reflux disease - The compound of the following formula:11-27-2008
20130165476OPTICALLY ACTIVE 2-HYDROXY TETRAHYDROTHIENOPYRIDINE DERIVATIVES, PREPARATION METHOD AND USE IN MANUFACTURE OF MEDICAMENT THEREOF - Optically active 2-hydroxytetrahydrothienopyridine derivatives represented by Formula I and pharmaceutically acceptable salts, preparation method and use in the manufacture of a medicament thereof are disclosed. The pharmacodynamic experiment results show that the present compounds of Formula I are useful for inhibiting platelet aggregation. The pharmacokinetic experiment results show that the present compound of Formula I can be converted in vivo into pharmacologically active metabolites and are therefore useful for inhibiting platelet aggregation. Therefore, the present compounds are useful for the manufacture of a medicament for preventing or treating thrombosis and embolism related diseases.06-27-2013
20130165477INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY - This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.06-27-2013
20110028514Azoles as Malonyl-CoA Decarboxylase Inhibitors Useful as Metabolic Modulators - The present invention relates to methods of treatment of certain metabolic diseases, and to novel compounds and their prodrugs, and/or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, this invention relates to the use of novel compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the formulae (I) and (II), wherein Y, C, R02-03-2011
20110003846POLYMORPH AND AMORPHOUS FORM OF (S)-(+)-CLOPIDOGREL BISULFATE - The present invention relates to new polymorphs of S-(+)-Clopidogrel bisulfate and a process for preparing the same.01-06-2011
20100130541Processes for the preparation of clopidogrel - The invention relates to processes for the preparation of clopidogrel and salts thereof. The inventors have developed a process for preparing racemic clopidogrel by racemizing R(−) clopidogrel. The process includes the step of reacting R(−) clopidogrel with a powered anhydrous base in one or more solvents.05-27-2010
20110124675THE HYDROSULFATE OF PRASUGREL, ITS PHARMACEUTICAL COMBINATION AND USE THEREOF - The present invention provides the prasugrel bisulfate of formula (II) and pharmaceutical composition and use thereof. Prasugrel bisulfate of the present invention has good stability, oral absorbability, metabolic activity and platelet aggregation inhibition effect, and low toxicity, and is therefore a promising anticoagulant for preventing or treating diseases associated with thrombosis or embolism.05-26-2011
20110077266Diamine Derivatives - The present invention relates to diamine compounds which inhibit activated blood coagulation factor X and exhibit an anticoagulant effect and there uses for treating various diseases based on thromboembolism.03-31-2011
20110003847Prasugrel Salts with Improved Properties - Acid addition salts of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine with sulfuric acid or sulfonic acids, pharmaceutical compositions comprising the same and processes for the production thereof. The acid addition salts have a low toxicity.01-06-2011
20090042930PHARMACEUTICAL COMPOSITIONS CONTAINING CLOPIDOGREL BISULFATE - Provided is a pharmaceutical composition including clopidogrel bisulfate and a pregelatinized starch. The pharmaceutical composition in which the stability of clopidogrel bisulfate is significantly enhanced can be obtained by mixing clopidogrel bisulfate with the pregelatinized starch.02-12-2009
20080214599Use of Par-1/Par-4 Inhibitors for Treating or Preventing Vascular Diseases - Use of a compound of formula (I) or a compound selected from the group consisting of a prasugrel metabolite, clopidogrel, a clopidogrel metabolite, ticlopidine, a ticlopidine metabolite, cangrelor, a cangrelor metabolite, AZD-6140, and an AZD-6140 metabolite for the treatment of and/or prevention of coagulation induced vascular diseases and recurrence thereof in a patient in need thereof.09-04-2008
20090209576PHARMACEUTICAL COMPOSITION CONTAINING CLOPIDOGREL CAMPHORSULFONATE OR POLYMORPHIC FORMS THEREOF - A pharmaceutical composition of the present invention which comprises clopidogrel camphorsulfonate of formula (I) or its polymorphic forms as an active ingredient is useful for treating or preventing a platelet aggregation-associated disease.08-20-2009
20100113506COMPOSITION FOR PREVENTING OR TREATING THROMBUS- OR EMBOLUS- ASSOCIATED DISEASE - Provided is a composition for the prevention or treatment of a thrombus- or embolus-associated disease, which comprises, as active ingredients to be applied in combination, at least one selected from the group consisting of clopidogrel and its pharmaceutically acceptable salts and at least one selected from the group consisting of icosapentaenoic acid as well as its pharmaceutically acceptable salts and esters.05-06-2010
20120238599HETEROCYCLIC COMPOUNDS AS MEK INHIBITORS - The invention provides novel substituted heterocyclic compounds represented by Formula I and Formula II, or a pharmaceutically acceptable salt, solvate, polymorph, ester, tautomer or prodrug thereof, and a composition comprising these compounds. The compounds provided can be used as inhibitors of MEK and are useful in the treatment of inflammatory diseases, cancer and other hyperproliferative diseases. The invention further provides a method of treatment for inflammatory diseases, cancer and other hyperproliferative diseases in mammals, especially humans.09-20-2012
20100249180ISOTHIAZOLOPYRIDINONES USEFUL FOR THE TREATMENT OF (INTER ALIA) CYSTIC FIBROSIS - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.09-30-2010
20100249179Farnesoid X Receptor Agonists - The present invention provides novel isoxazole compounds, pharmaceutical compositions, therapeutic uses and processes for preparing the same.09-30-2010
20090054479FUSED HETEROCYCLIC DERIVATIVES AS PPAR MODULATORS - The present invention is directed to compounds represented by the following structural formula, Formula I:02-26-2009
20120108628INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY - This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling and HGF receptor signaling. More particularly, the invention relates to compounds, compositions and methods for the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.05-03-2012
20100081684METHODS FOR TREATING INFLAMMATORY DISORDERS - The invention described herein is based, in part, on the discovery that thieno[3,2-c]pyridine derivatives prevent inflammation in the setting of inflammatory disorders, such as asthma. Described herein are methods for treating inflammatory disorders including, for example asthma, by administering a thieno[3,2-c]pyridine derivative compound to an individual in need thereof.04-01-2010
20100081685PHARMACEUTICAL COMPOSITION - To provide pharmaceutical preparation exhibiting satisfactory dissolution property in a wide pH range.04-01-2010
20080207681DEVICE AND METHODS FOR IDENTIFYING AND TREATING ASPIRIN NON-RESPONSIVE PATIENTS - The present invention relates to methods and compositions for identifying and treating subjects in need of antithrombotic therapies but who are not responsive to aspirin.08-28-2008
20090281136PRASUGREL PHARMACEUTICAL FORMULATIONS - Pharmaceutical formulations comprising prasugrel, including its pharmaceutically acceptable salts, hydrates, solvates, polymorphs, and mixtures thereof. Also described are processes for preparing the stable formulations and their methods of use.11-12-2009
20110207767Novel cc-1065 Analogs and Their Conjugates - This invention relates to novel analogs of the DNA-alkylating agent CC-1065 and to their conjugates. Furthermore this invention concerns intermediates for the preparation of said agents and conjugates. The conjugates are designed to release their (multiple) payload after one or more activation steps and/or at a rate and time span controlled by the conjugate in order to selectively deliver and/or controllably release one or more of said DNA alkylating agents. The agents, conjugates, and intermediates can be used to treat an illness that is characterized by undesired (cell) proliferation. As an example, the agents and the conjugates of this invention may be used to treat a tumor.08-25-2011
20080280948MODULATORS OF AMYLOID BETA - The invention relates to compounds of formula11-13-2008
20090264460CLOPIDOGREL PHARMACEUTICAL FORMULATIONS - Formulations of clopidogrel or pharmaceutically acceptable salts thereof, processes of preparation of such formulations, and methods of using them.10-22-2009
20090149495COMPOUNDS - The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I) wherein X represents a group selected from CO, SO, SO06-11-2009
20120196891HETEROCYCLIC COMPOUND AND ITS USE FOR CONTROL OF AN ARTHROPOD PEST - A heterocyclic compound represented by formula (1): 08-02-2012
20090163536METHODS AND COMPOUNDS FOR TREATMENT OF CLOSTRIDIUM BASED INFECTION - Methionyl tRNA synthetase inhibitors (MetRS) are provided for use in therapy as antibacterial agents in 06-25-2009
20090163538Tetrahydropyridothiophenes For Use In The Treatment Of Cancer - Compounds of formula (I), in which Ra and Rb have the meanings indicated in the description, are novel effective compounds with anti-proliferative and/or apoptosis inducing activity.06-25-2009
20090163537Thienopyridinone Compounds and Methods of Treatment - The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.06-25-2009
20090118323ANTITUMOR BENZOYLSULFONAMIDES - The present invention provides antitumor compounds of the formula (I); and antitumor methods.05-07-2009
20090326002Thieno [2,3-b] Pyridine Compounds with mGluR Activity - Provided herein are Thieno[2,3-b]pyridine compounds with mGluR activity. Also provided herein are processes and intermediates for the preparation of the Thieno[2,3-b]pyridine compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in treatment, therapy, and/or prevention of conditions which require modulation of mGluR1 and mGluR5 receptors.12-31-2009
20090082391NOVEL AMINOALCOHOL-SUBSTITUTED ARYLDIHYDROISOQUINOLINONES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS MEDICAMENTS - The invention relates to aminoalcohol-substituted aryldihydroisoquinolinones and their derivatives, and their physiologically tolerated salts and physiologically functional derivatives, their preparation, medicaments comprising at least one aminoalcohol-substituted aryldihydroisoquinolinone of the invention or its derivative, and the use of the aminoalcohol-substituted aryldihydroisoquinolinones of the invention and their derivatives as MCH antagonists.03-26-2009
20080262028IMIDAZOLE DERIVATIVES AS INHIBITORS OF TAFIA - The present invention is directed to a compound of formula I:10-23-2008
20090221630IAP INHIBITORS - The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula (I): wherein Q, X09-03-2009
20090048287Compositions useful for treating gastrointestinal motility disorders - The present invention relates to method of treating a gastrointestinal motility disorder in a subject in need of treatment comprising coadministering to said subject a first amount of a compound having 5-HT02-19-2009
20090048286Inhibitors of Protein Tyrosine Phosphatase 1B - Protein tyrosine phosphatases (PTPases) such as PTP1B can play a role in regulating a wide variety of cellular responses such as insulin signaling. Substituted bicyclic fused-thiophene compounds can inhibit PTP1B and thereby induce greater insulin sensitivity. Accordingly, PTP1B inhibition can provide an alternate treatment for PTPase-mediated disorders such as diabetes.02-19-2009
20110060001THIENOPYRIDONE DERIVATIVES AS AMP- ACTIVATED PROTEIN KINASE (AMPK) ACTIVATORS - The present invention relates to compounds of formula (I) wherein R03-10-2011
201002223782-HETEROARYLCARBOXYLIC ACID AMIDES - The invention relates to novel 2-heteroarylcarboxamides, processes for their preparation, and their use for producing medicaments for the treatment and/or prophylaxis of diseases and for improving perception, concentration, learning and/or memory.09-02-2010
20100227882CLOPIDOGREL SALT AND POLYMORPHIC FORMS THEREOF - The invention relates to methyl(+)-(S)-α-(2-chlorophenyl)-6,7-dihydrothieno[3,2-C]pyridine-5(4H) acetate naphthalene-1,5-disulfonate or a polymorphic form and/or a hydrate and/or a solvate thereof, to pharmaceutical compositions containing the same, and to the method of use thereof for inhibiting platelet aggregation.09-09-2010
20090076067PHARMACEUTICAL COMPOSITION COMPRISING AZARHODACYANINE COMPOUND AS ACTIVE INGREDIENT - The object of the invention is to provide pharmaceutical composition that can be used as a therapeutic and/or prophylactic agent. Particularly, the pharmaceutical composition of the invention has significant therapeutic effect and survival benefit for the disease caused by parasitic protozoa, and selective toxicity against the causative protozoa. The pharmaceutical composition comprises a compound represented by general formula (1). Particularly, the invention relates to a composition that is an effective therapeutic/prophylactic agent for malaria, 03-19-2009
20130137716PARENTERAL DEXTROSE FORMULATION OF CLOPIDOGREL - Described herein are ways to solubilize clopidogrel for parenteral administration containing clopidogrel and D05-30-2013
20110034505THIENOPYRIDONE DERIVATIVES AS AMP-ACTIVATED PROTEIN KINASE (AMPK) ACTIVATORS - The present invention relates to compounds of formula (I) wherein R1, R2 and R3 are as defined in claim 02-10-2011
20110034504AGENT FOR PREVENTING AND/OR TREATING VASCULAR DISEASES - [Object] To provide an excellent pharmaceutical composition for preventing and/or treating vascular diseases.02-10-2011
20110082170THIENOPYRIDYL COMPOUNDS THAT INHIBIT VANILLOID RECEPTOR SUBTYPE 1 (VR1) AND USES THEREOF - The present invention discloses fused thienopyridyl compounds of general formula (I)04-07-2011
20100056564Association of an anti-atherothrombotic agent and an anti-platelet-aggregation agent - The present invention relates to a new association of an anti-atherothrombotic agent and an anti-platelet-aggregation agent.03-04-2010
20120202844Crystal Forms of Kinase Inhibitors - Citrate salts of N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N′-(3-fluorophenyl)urea and crystalline forms thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.08-09-2012
20110053973COMPOUNDS AS TYROSINE KINASE MODULATORS - The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.03-03-2011
20110077265INHIBITORS OF IAP - The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1-M-U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3′, R4, R4′ and R5, are as described herein.03-31-2011
20100298370BENZOTHIAZOLYL THIENOPYRIDINE DERIVATIVES AND USES THEREOF - Novel benzothiazolyl thienopyridine compounds are provided and pharmaceutical compositions comprising benzothiazolyl thienopyridine compounds. The benzothiazolyl thienopyridine compounds are capable of inhibiting the interactions between vascular endothelial growth factor (VEGF) and heparan sulfate glycosaminoglycans (HS-GAGs), and are useful for prevention or treatment of diseases and disorders such as inflammation, autoimmune diseases and cancer.11-25-2010
20100179185Novel Aminothienopyridinone Derivatives Processes for Preparing Them and Pharmaceutical Compositions Thereof - The present invention concerns novel 3-aminothienopyridinone derivatives of the formula I, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.07-15-2010
20110136858Preferred Combination Therapy - Composition and use of a medicament comprising a fixed dose combination of droloxifene and clopidogrel, or the pharmaceutically acceptable salts thereof, for treating or preventing a disorder associated with the loss of normal adult tissue architecture.06-09-2011
20090176825PROLYL HYDROXYLASE INHIBITORS - The invention described herein relates to certain bicyclic heteroaromatic N-substituted glycine derivatives of formula (I)07-09-2009
20100016350NOVEL MCH RECEPTOR ANTAGONISTS - The present invention relates to a melanin concentrating hormone antagonist compound of formula (I): wherein R01-21-2010
20110118303NOVEL COMPOUNDS DERIVED FROM TAURINE, PROCESS OF THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THESE - The present invention relates to compounds derived from taurine with non-steroidal anti inflammatory activity.05-19-2011
20090203729Process for Producing High-Purity Prasugrel and Acid Addition Salt Thereof - The present invention is directed to providing prasugrel hydrochloride or the like with a reduced content of OXTP. A method for producing prasugrel hydrochloride with a reduced content of OXTP, comprising dissolving free prasugrel containing OXTP in an inert solvent and adding hydrochloric acid optionally dropwise to the solution for reaction is also provided.08-13-2009
20090270448PHARMACEUTICAL FORMULATIONS COMPRISING CLOPIDOGREL - Melt granulate in the form of a solid state dispersion of the drug in a pharmaceutically acceptable carrier, wherein said melt granulate comprises a pharmaceutically active compound, preferably clopidogrel, at least one carrier material, and optionally pharmaceutically acceptable excipients and method of making said melt granulate.10-29-2009
20110118302PREPARATION AND USE OF BIPHENYL-4-YL-CARBONYLAMINO ACID DERIVATIVES FOR THE TREATMENT OF OBESITY - This invention relates to certain biphenyl-4-yl carbonylamino acid compounds, compositions, and methods for treating or preventing obesity and related diseases.05-19-2011
20090247569Process for Preparing Clopidogrel Bisulphate - Provided are processes for the preparation of clopidogrel bisulphate Form I.10-01-2009
20100144783KINASE INHIBITORS WITH IMPROVED CYP SAFETY PROFILE - Compounds that inhibit protein kinases such as Aurora-kinases and the VEGFR and PDGFR families of kinases, with an improved safety profile due to low CYP3A4 inhibition, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.06-10-2010
20120149726Crystal Forms of Kinase Inhibitors - N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N′-(3-fluorophenyl)urea free base and crystallines form thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.06-14-2012
20100280064PHARMACEUTICAL COMPOSITION HAVING IMPROVED STORAGE STABILITY - A pharmaceutical composition containing (A) a compound represented by the formula (I) below or a pharmacologically acceptable salt thereof, and (B) a water-soluble polymer. The formula (I) is as follows:11-04-2010
20100179184ARTICLE OF MANUFACTURE FOR PRASUGREL - An article of manufacture comprising packaging prasugrel tablets, caplets, capsule or other solid form of prasugrel in an air and/or moisture impervious container under a positive liquid gas pressure.07-15-2010
20090069369DEUTERIUM-ENRICHED PRASUGREL - The present application describes deuterium-enriched prasugrel, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-12-2009
20120004256PARENTERAL FORMULATION OF CLOPIDOGREL - Described herein are ways to solubilize clopidogrel for parenteral administration containing clopidogrel and a diluent NNDMA (N,N-dimethylacetamide); useful in the prevention of platelet aggregation in acute coronary syndrome, acute myocardial infarction or to prevent platelet facilitated thrombosis following coronary angioplasty and/or coronary stenting.01-05-2012
20120252837BICYCLIC DERIVATIVES OF AZABICYCLIC CARBOXAMIDES, PREPARATION THEREOF AND THERAPEUTIC USE THEREOF - The disclosure relates to compounds of formula (I):10-04-2012
20120015976AUTOTAXIN INHIBITORS - The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.01-19-2012
20120309783KINASE INHIBITORS WITH IMPROVED CYP SAFETY PROFILE - Compounds that inhibit protein kinases such as Aurora-kinases and the VEGFR and PDGFR families of kinases, with an improved safety profile due to low CYP3A4 inhibition, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.12-06-2012
20100093785DIAMINE DERIVATIVES - A compound represented by the general formula (1):04-15-2010
20110184014NEW COMPOUNDS - The present invention relates to new mGluR1 and mGluR5 receptor subtype preferring ligands of formula (I); wherein Y represents a substituent selected from hydrogen, methyl, fluoro, chloro, bromo, methoxy; Z is hydrogen or methyl; R is an optionally substituted heteroaryl, and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluR1 and mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain and neuromuscular dysfunctions of the lower urinary tract.07-28-2011
20100204268PROCESSES FOR PREPARING DIFFERENT FORMS OF (S)-(+)-CLOPIDOGREL BISULFATE - The invention provides improved processes for the preparation of hydrated form of (S)-(+)-Clopidogrel bisulfate as well as improved processes for the preparation of form-I and form-II of (S)-(+)-Clopidogrel bisulfate.08-12-2010
20100173933ANTIBACTERIAL AGENTS - Compounds of formula (I) have antibacterial activity:07-08-2010
20120178777Medicaments for Inhibiting Thrombus Formation - A Medicaments for inhibiting thrombus formation contains active ingredients which are triflusal and clopidogrel bisulfate, wherein a mass ratio of triflusal to clopidogrel bisulfate is (100-650):(30-150), preferably (1-20):1, more preferably (3-6):1, and even more preferably 3:1 or 6:1.07-12-2012
20120122918ANTIBACTERIAL AGENTS - Compounds of formula (1) have antibacterial activity:05-17-2012
20090326001THIENOPYRIDINE DERIVATIVES AS MODULATORS OF METABOTROPIC GLUTAMATE RECEPTORS - The present invention relates to new mGluR1 and niGluR5 receptor subtype preferring ligands of formula (I): wherein X represents a group selected from (CH12-31-2009
20120190708TARGETING NAD BIOSYNTHESIS IN BACTERIAL PATHOGENS - The emergence of multidrug-resistant pathogens necessitates the search for new antibiotics acting on previously unexplored targets. Nicotinate mononucleotide adenylyltransferase of the NadD family, an essential enzyme of NAD biosynthesis in most bacteria, was selected as a target for structure-based inhibitor development. To this end, the inventors have identified small molecule compounds that inhibit bacterial target enzymes by interacting with a novel inhibitory binding site on the enzyme while having no effect on functionally equivalent human enzymes.07-26-2012
201101246745/5-OR 5/6-MEMBERED CONDENSED RING CYCLOALKYLAMINE DERIVATIVE - Disclosed are a compound of a formula (I) and its pharmaceutically-acceptable salt:05-26-2011
20100204267Preventive and therapeutic medicament for gastroesophageal reflux disease - The compound of the following formula:08-12-2010
20100168158MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.07-01-2010
20100168157PREVENTIVE AND THERAPEUTIC MEDICAMENT FOR GASTROESOPHAGEAL REFLUX DISEASE - The compound of the following formula:07-01-2010
20100168156Novel Benzoxathiine Derivative - Disclosed is a compound represented by the formula (I) below and a pharmaceutically acceptable salt thereof.07-01-2010
20130012534Pharmaceutical Compositions Comprising Prasugrel and Cyclodextrin Derivatives and Methods of Making and Using the Same - The present invention is directed to pharmaceutical compositions comprising prasugrel and a cyclodextrin derivative, and methods of making and using the same.01-10-2013
20130012535SUSTAINED-RELEASE SOLID PREPARATION FOR ORAL USE - It is intended to avoid dose dumping of a drug and improve the dissolution properties of the drug in the lower gastrointestinal tract, and thereby provide a sustained-release pellet preparation for oral administration that reliably exhibits its main pharmacological effect when orally administered once or twice a day. The present invention provides a sustained-release preparation obtained by mixing of (A) a pharmacologically active drug, (B) hydroxypropyl methylcellulose acetate succinate, (C) a plasticizer, and (D) polyethylene glycol followed by extrusion granulation.01-10-2013
20120149727PRASUGREL IN NON-CRYSTALLINE FORM AND PHARMACEUTICAL COMPOSITION THEREOF - The present invention relates to prasugrel or a pharmaceutically compatible salt thereof, compositions that contain this active substance and pharmaceutical compositions that contain this active substance or a composition containing this active substance. The present invention further relates to methods for producing the novel compositions.06-14-2012
20130023556AUTOTAXIN INHIBITORS - The present invention relates to compounds according to formula (I) as autotaxin inhibitors and the use of such compounds for the treatment and/or prophylaxis of physiological and/or pathophysiological conditions, which are caused, mediated and/or propagated by increased lysophosphatic acid levels and/or the activation of autotaxin, in particular of different cancers.01-24-2013
20130023555KINASE INHIBITOR WITH IMPROVED SOLUBILITY PROFILE - 4-Amino-N-[3-(diethylamino)propyl]-3-(4-{[(3-fluorophenyl)carbamoyl]amino}phenyl)thieno[3,2-c]pyridine-7-carboxamide which inhibits protein kinases such as Aurora-kinases and the VEGFR and PDGFR families of kinases, with an improved aqueous solubility profile, compositions containing 4-amino-N-[3-(diethylamino)propyl]-3-(4-{[(3-fluorophenyl)carbamoyl]amino}phenyl)thieno[3,2-c]pyridine-7-carboxamide and methods of treating diseases using 4-amino-N-[3-(diethylamino)propyl]-3-(4-{[(3-fluorophenyl)carbamoyl]amino}phenyl)thieno[3,2-c]pyridine-7-carboxamide are disclosed.01-24-2013
20080255184Thienopyridine B-Raf Kinase Inhibitors - The present invention provides thienopyridine compounds, compositions containing the same, as well as processes for the preparation and their use as pharmaceutical agents.10-16-2008
20080227808Substituted Phenylether-Thienopyridone Compounds With Antibacterial Activity - Novel bicyclic heteroaromatic compounds are provided that are inhibitors of bacterial methionyl tRNA synthetase (MetRS). Compounds of the invention generally have a left hand side phenylether constituent and a right hand side thienopyridone constituent. Also disclosed are methods for their preparation and their use in therapy as antibacterial agents, particularly as anti-09-18-2008
20110269792COMPOSITIONS USEFUL FOR TREATING IRRITABLE BOWEL SYNDROME - The present invention relates to a method of treating irritable bowel syndrome with constipation (IBS-c) or irritable bowel syndrome with alternating constipation and diarrhea (IBS-a) in a subject in need of treatment. The method comprises administering to said subject a therapeutically effective amount of a thieno[3,2-b]pyridine compound of Structural Formula I or a pharmaceutically acceptable salt or N-oxide derivative thereof.11-03-2011
20130096154METHODS AND COMPOSITIONS FOR THE ASSESSMENT OF DRUG RESPONSE - The present invention provides methods for predicting or determining a subject's response to an antiplatelet agent, and methods for determining a subject's suitability to a treatment regime or intervention for a disease associated with platelet aggregation, using analysis of genetic polymorphisms. The present invention also relates to the use of genetic polymorphisms in assessing a subject's response to an antiplatelet agent. Nucleotide probes and primers, kits, and microarrays suitable for such assessment are also provided04-18-2013
20130096153METHODS AND COMPOSITIONS FOR THE ASSESSMENT OF DRUG RESPONSE - The present invention provides methods for predicting or determining a subject's response to an antiplatelet agent, and methods for determining a subject's suitability to a treatment regime or intervention for a disease associated with platelet aggregation, using analysis of genetic polymorphisms. The present invention also relates to the use of genetic polymorphisms in assessing a subject's response to an antiplatelet agent. Nucleotide probes and primers, kits, and microarrays suitable for such assessment are also provided04-18-2013
20080200497Hepatitis C Inhibitor Peptide Analogs - The compounds of formula I wherein R08-21-2008
20110224251Therapeutic Pyrazolyl Thienopyridines - The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof,09-15-2011
20110275667COMPOSITIONS USEFUL FOR TREATING GASTROESOPHAGEAL REFLUX DISEASE - The present invention relates to a method of treating GERD in a human subject in need of treatment. The method comprises orally administering to said subject an effective amount of a thieno[3,2-b]pyridine compound of Structural Formula I or a pharmaceutically acceptable salt or N-oxide derivative thereof, wherein the effective amount is from about one to about three daily doses of the compound and the dose is from about 0.2 mg to about 0.5 mg.11-10-2011
20110275666ACTIVATED BLOOD COAGULATION FACTOR X (FXA) INHIBITOR - An object of the present invention is to provide an activated blood coagulation factor X (FXa) inhibitor that reduces the risk of bleeding caused by the treatment of thromboembolism. The present invention provides an oral anticoagulant agent comprising a compound represented by the following formula (1):11-10-2011
20110237620HETEROCYCLIC COMPOUND AND USE THEREOF - A compound represented by formula (I) or a salt thereof, which has a potent Raf inhibitory activity.09-29-2011
20100292268Formulations Containing Clopidogrel and Sulfoalkyl Ether Cyclodextrin and Methods of Use - The present invention provides compositions containing clopidogrel, present as a free base or a pharmaceutically acceptable salt thereof, and sulfoalkyl ether cyclodextrin (SAE-CD). The compositions can be liquid, suspension or solid compositions. They can be adapted for oral, peroral or parenteral administration. The SAE-CD serves to aid in dissolution and stabilization of the clopidogrel in aqueous media. The stability of clopidogrel against hydrolytic degradation, thermal degradation, and photolytic degradation are improved. SAE-CD provides improved results over other cyclodextrin derivatives. The SAE-CD-containing composition of clopidogrel can be provided in liquid form, solid form or as a reconstitutable powder. Both ready-to-use and concentrated liquid compositions can be prepared. The liquid composition is optionally available as a clear solution. The compositions herein can be administered perorally or parenterally and provide substantial pharmacokinetic, pharmacodynamic and/or therapeutic advantages over a tablet composition administered perorally and excluding SAE-CD.11-18-2010
20130158069PREVENTIVE AND/OR THERAPEUTIC AGENT FOR THROMBOEMBOLISM IN THROMBOEMBOLISM PATIENT WITH SEVERE RENAL IMPAIRMENT - It is intended to provide a highly safe, orally administrable preventive and/or therapeutic agent for thrombosis and/or embolism that can be applied to a thrombosis and/or embolism patient with severe renal impairment. The present inventors have found that even for a thrombosis and/or embolism patient with severe renal impairment, use of edoxaban at a dose of 15 mg once a day can effectively prevent thrombosis and/or embolism while avoiding the risk of bleeding. The present inventors have also found that even for a thrombosis and/or embolism patient with severe renal impairment, edoxaban at a dose of 15 mg once a day can effectively prevent thrombosis and/or embolism with safety over a long period.06-20-2013
20130184308ACTIVATED BLOOD COAGULATION FACTOR X (FXa) INHIBITOR - An object of the present invention is to provide an activated blood coagulation factor X (FXa) inhibitor that reduces the risk of bleeding caused by the treatment of thromboembolism. The present invention provides an oral anticoagulant agent comprising a compound represented by the following formula (07-18-2013
20110312991ACTIVATED BLOOD COAGULATION FACTOR INHIBITOR - An object of the present invention is to provide a novel salt form of a compound that exhibits an inhibitory effect on activated blood coagulation factor X, and is useful as a preventive and/or therapeutic drug for thrombotic diseases, and crystals thereof. The present invention provides N12-22-2011
20110312990Diamine Derivatives - A compound represented by the general formula (1):12-22-2011
20120035206PREPARATION AND APPLICATION OF NOVEL ANTIBACTERIAL AND ANTICANCER COMPOUNDS AND THEIR DERIVATIVES - Novel antibiotic and anticancer compounds of formula I, II, III, IV, derivatives, ostereoisomer, racemic and noracemic mixture of ostereoisomer, or the pharmaceutically acceptable salts or solvates of these compounds are disclosed. The preparation, pharmaceutical composition and biological activity of these compounds are disclosed.02-09-2012
20120095035CRYSTALS OF PRASUGREL HYDROBROMATE - The present application discloses crystals of 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine hydrobromate, crystal compositions and pharmaceutical compositions comprising them and their use. The crystals of prasugrel hydrobromate of the present application possess excellent stability and solubility.04-19-2012

Patent applications in class Ring sulfur in the bicyclo ring system