| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 540596000 | Additional hetero ring attached directly or indirectly to the hetero ring by nonionic bonding | 41 |
| 20080269481 | Compounds and methods for the treatment or prevention of Flavivirus infections - Compounds represented by formula: | 10-30-2008 |
| 20100249400 | NOVEL DIHYDRONAPHTHALENE COMPOUND AND USE THEREOF - Disclosed is a compound represented by the formula (I) below as a dihydronaphthalene compound having a chemical structure which is excellent in production efficiency when compared with lasofoxifene and nafoxidine. This compound is useful as a proteasome inhibitor and/or an antitumor agent. | 09-30-2010 |
| 20140309418 | Gambogenic Acid Derivatives, Preparation Method and Application Thereof - Gambogenic acid derivatives having a structure shown as Formula (I) or (II), salts, preparation method and application thereof in the treatment of tumor. Compared with gambogenic acid, the gambogenic acid derivatives exhibit more potent anti-tumor activities. | 10-16-2014 |
| 540597000 | The additional hetero ring is six-membered and contains nitrogen | 23 |
| 20080262224 | Method of Preparation of Benzofuran-2-Carboxylic Acid -Amide - This invention relates to a method of preparation of benzofuran-2-carboxylic acid {(S)-3-methyl- | 10-23-2008 |
| 20080262225 | Use of metal complex compounds as oxidation catalysts - Use of metal complex compounds of formula | 10-23-2008 |
| 20090069559 | Compositions and methods for modulating sirtuin activity - The present invention is based, in part, on our discovery of compounds that inhibit an activity of a sirtuin (e.g., compounds that inhibit or preferentially inhibit an activity of SIRT2) and are therefore believed useful in the treatment or prevention of diseases associated with sirtuin activity. These diseases include, but are not limited to, neurological disorders such as Parkinson's Disease (PD). | 03-12-2009 |
| 20090281308 | CHEMOKINE RECEPTOR BINDING HETEROCYCLIC COMPOUNDS WITH ENHANCED EFFICACY - Compounds that interact with the CXCR4 receptor are described. These compounds are useful in treating, for Example, HIV infection and inflammatory conditions such as rheumatoid arthritis, as well as asthma or cancer, and are useful in methods to elevate progenitor and stem cell counts as well as methods to elevate white blood cell counts. | 11-12-2009 |
| 20100029936 | Quinolone Carboxylic Acids, Derivatives Thereof, and Methods of Making and Using Same - A process of preparing a quinolone carboxylic acid or its derivatives having Formula I, Ia, Ib, or IV, as shown herein, comprises using a starting quinolone that already has one or more desired substituents at one or more particular positions on the quinolone ring and preserving the orientation of such substituents throughout the synthesis. The present process comprises fewer steps than prior-art processes. The present process also can include a simple separation of a desired enantiomer of the quinolone carboxylic acid or its derivatives from the enantiomeric mixture. Pharmaceutical compositions comprising fluoroquinolones prepared by the present process can be used effectively against a variety of microbial pathogens. | 02-04-2010 |
| 20100121051 | UROTENSIN II RECEPTOR ANTAGONISTS - Compounds of the formula (I) | 05-13-2010 |
| 20100168417 | 2-Indolyl Imidazo [4,5-d] Phenanthroline Derivatives and Their Use in the Treatment for Cancer - 2-indolyl imidazo[4,5-d]phenanthroline compounds of Formula I that are capable of intracellular chelation of transition metals and of exerting antiproliferative effects in cancer cells, that are cytostatic and/or cytotoxic, are provided. Compounds of Formula I can also induce apoptosis in cancer cells and are thus capable of exerting a cytotoxic effect on cancer cells. The compounds of Formula I are also capable of selectively inhibiting the proliferation of one or more of prostate cancer cells, colon cancer cells, non-small lung cancer cells and leukemia cells. The compounds of Formula I are also capable of increasing the expression of the zinc-regulated tumour suppressor, KLF4 and thus are useful in inhibiting the proliferation of cancer cells in which KLF4 functions as a tumour-suppressor, including, but not limited to, bladder cancer, cancers of the gastrointestinal tract and various leukemias. | 07-01-2010 |
| 20100210836 | SMALL MOLECULE INHIBITORS OF LYMPHOID TYROSINE PHOSPHATASE - The present invention relates to lymphoid tyrosine phosphatase inhibitors and autoimmunity. More specifically, the invention relates to the identification of lymphoid tyrosine phosphatase inhibitors and the analysis of the structure-activity relationship. | 08-19-2010 |
| 20120245344 | GPR119 AGONIST - A compound represented by the formula (II) is a GPR119 agonist, and is used as an agent for treating diabetes: | 09-27-2012 |
| 20120289696 | THIAZOLYL MGLUR5 ANTAGONISTS AND METHODS FOR THEIR USE - The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts. | 11-15-2012 |
| 20130046093 | PHARMACEUTICAL COMPOSITIONS FOR PREVENTING OR TREATING DEGENERATIVE BRAIN DISEASE AND METHOD OF SCREENING THE SAME - A pharmaceutical composition for preventing or treating a degenerative brain disease, and a method of screening a material for preventing or treating a degenerative brain disease. The method may effectively screen a prophylactic or therapeutic candidate material for preventing or treating a degenerative brain disease. A variety of degenerative brain diseases may be effectively prevented or treated using the pharmaceutical composition including a screened material for preventing or treating a degenerative brain disease. | 02-21-2013 |
| 20130211075 | AMIDE DERIVATIVE AND USE THEREOF - The present invention relates to a novel amide derivative. More specifically, the present invention provides a medicinal agent useful as a prophylactic or therapeutic agent for diseases, which relies on the production of cytokines from T cells, and which comprises an amide derivative or a pharmacologically acceptable salt thereof or a solvate of the derivative or the pharmacologically acceptable salt as an active ingredient. Provided is an amide derivative represented by general formula (I) | 08-15-2013 |
| 20130267700 | ALKYLAMINE-SUBSTITUTED DICYANOPYRIDINE AND AMINO ACID ESTER PRODRUGS THEREOF - The present application relates to novel 6-alkylamino-substituted dicyanopyridines, to their amino acid ester prodrugs, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders. | 10-10-2013 |
| 20130310557 | Amorphous Besifloxacin Solid - Amorphous solid-state form of (R)-(+)-7-(3-amino-2,3,4,5,6,7-hexahydro-1H-azepin-1-yl)-1-cyclopropyl-8-chloro-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid is characterized by at least one of: (a) an X-ray powder diffraction (“XRPD”) spectrum that comprises peaks at 2θ angles of 6.9-7.1, 9.4, 10.6-10.7, and 13.4-13.7°±0.2°, and a diffuse halo pattern at 11-30°; and (b) a DSC (differential scanning calorimetry) melting peak at about 267-272° C. The amorphous solid is prepared by rapid precipitation from a saturated or supersaturated solution of besifloxacin free base in a solvent comprising at least benzyl alcohol. | 11-21-2013 |
| 20140243520 | PYRROLOPYRIDINES AS KINASE INHIBITORS - Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 08-28-2014 |
| 20140296515 | ALKYLAMINE-SUBSTITUTED DICYANOPYRIDINE AND AMINO ACID ESTER PRODRUGS THEREOF - The present application relates to novel 6-alkylamino-substituted dicyanopyridines, to their amino acid ester prodrugs, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of cardiovascular disorders. | 10-02-2014 |
| 540598000 | Plural hetero atoms in the additional hetero ring | 7 |
| 20150025235 | Benzamide Compounds and Related Methods of Use - Benzamide compounds and derivatives thereof, as can be used for selective inhibition of the SIRT2 enzyme and/or therapeutic use in the treatment of Huntington's disease. | 01-22-2015 |
| 540599000 | Polycyclo ring system having the additional hetero ring as one of the cyclos | 2 |
| 540600000 | The additional hetero ring is 1,3-diazine (including hydrogenated) | 2 |
| 20100190977 | 4-PHENYLAMINO-QUINAZOLIN-6-YL-AMIDES - This invention provides quinazoline compounds of the formula: | 07-29-2010 |
| 20120238751 | TRICYCLIC GYRASE INHIBITORS - Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. | 09-20-2012 |
| 540601000 | The additional hetero ring is 1,3-diazine (including hydrogenated) | 4 |
| 20090203903 | Thiazolyl mglur5 antagonists and methods for their use - The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts. | 08-13-2009 |
| 20090264649 | DIARYLAMINE-CONTAINING COMPOUNDS AND COMPOSITIONS, AND THEIR USE AS MODULATORS OF C-KIT RECEPTORS - Described herein are compounds that include a diarylamine structural feature. Also described herein are methods for making such compounds, methods for using such compounds to modulate the activity of c-kit receptors, and pharmaceutical compositions and medicaments comprising such compounds. Also described herein are methods of using such compounds, pharmaceutical compositions and medicaments to treat and/or prevent and/or inhibit and/or ameliorate the pathology and/or symptomology diseases or conditions associated with the activity of c-kit receptors. | 10-22-2009 |
| 20090275750 | DIPEPTIDYL PEPTIDASE INHIBITORS - Methods of making compounds of the formula (I) wherein the variables are as defined herein. Also, methods of making compounds that may be used to inhibit dipeptidyl peptidase. | 11-05-2009 |
| 20100036117 | PYRIMIDINE COMPOUND AND PESTS CONTROLLING COMPOSITION CONTAINING THE SAME - The present invention relates to a pyrimidine compound of the formula (II′): | 02-11-2010 |
| 540602000 | The additional hetero ring is five-membered and contains nitrogen | 15 |
| 20080249302 | SUBSTITUTED INDOLE COMPOUNDS HAVING NOS INHIBITORY ACTIVITY - The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing conditions such as, for example, stroke, reperfusion injury, neurodegeneration, head trauma, CABG, migraine headache with and without aura, migraine with allodynia, central post-stroke pain (CPSP), neuropathic pain, morphine/opioid induced tolerance and hyperalgesia. | 10-09-2008 |
| 20080249303 | METHODS OF SEPARATION AND DETECTION OF BAZEDOXIFENE ACETATE IN PHARMACEUTICAL COMPOSITIONS - Methods are disclosed for separating and detecting bazedoxifene acetate from pharmaceutical compositions containing a mixture of bazedoxifene acetate and one or more other components that produce X-Ray diffraction patterns having interfering peaks at or near the characteristic peaks for bazedoxifene acetate. | 10-09-2008 |
| 20080255350 | SUBSTITUTED AZA-INDOLES AS INHIBITORS OF POLY(ADP-RIBOSE) POLYMERASE (PARP) - The present invention relates to a series of substituted aza-indole derivatives of the formula I: | 10-16-2008 |
| 20100016581 | METHODS OF PREPARING POLYMORPHIC FORM A OF BAZEDOXIFENE ACETATE - The present invention relates to methods of preparing polymorphic Form A of bazedoxifene acetate and polymorphic Form A prepared by such methods. | 01-21-2010 |
| 20100016582 | METHODS OF CONVERTING POLYMORPHIC FORM B OF BAZEDOXIFENE ACETATE TO POLYMORPHIC FORM A OF BAZEDOXIFENE ACETATE - The present invention relates to methods of preparing polymorphic Form A of bazedoxifene acetate and polymorphic Form A prepared by such methods. | 01-21-2010 |
| 20100240888 | SALTS OF BAZEDOXIFENE - The invention deals with new crystalline salts of bazedoxifene, by means of which a high API quality can be achieved in a high yield. | 09-23-2010 |
| 20120253038 | PROCESSES FOR THE SYNTHESIS OF BAZEDOXIFENE ACETATE AND INTERMEDIATES THEREOF - Efficient processes for the synthesis of pharmaceutically useful compounds such as (1-[4-(2-azepan-1-yl-ethoxy)-benzyl]-2-(4-hydroxy-phenyl)-3-methyl-1H-indol-5-ol acetic acid commonly known as bazedoxifene acetate (Formula IX) using cyanomethoxybenzyl halides of Formula III, where X=Halogens e.g., Cl, F, Br, I; G=Any electron donating or electron withdrawing substituent. | 10-04-2012 |
| 20120330008 | NOVEL PROCESS FOR THE PREPARATION OF BAZEDOXIFENE ACETATE AND INTERMEDIATES THEREOF - A novel process is described for the preparation of pharmaceutically useful compounds such as 1-{4-[2-(azepan-1-yl)ethoxy]benzyl}-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetic acid commonly known as bazedoxifene acetate of the formula-1 using 2-(4-{[5-(benzyloxy)-2-[4-(benzyloxy)phenyl]-3-methyl-1H-indol-1-yl]methyl}phenoxy)ethyl-4-methylbenzenzene-1-sulfonate (formula 2a) | 12-27-2012 |
| 20130018184 | METHODS OF PREPARING POLYMORPHIC FORM A OF BAZEDOXIFENE ACETATE - The present invention relates to methods of preparing polymorphic Form A of bazedoxifene acetate and polymorphic Form A prepared by such methods. | 01-17-2013 |
| 20130225805 | PREPARATION OF CRYSTALLINE BAZEDOXIFENE AND ITS SALTS - Aspects of the present disclosure include crystalline bazedoxifene free base, crystalline bazedoxifene acetate Form D, and processes for their preparation. The drug compound having the adopted name “bazedoxifene acetate” has a chemical name 1-[4-(2-azepan-1-yl-ethoxy)benzyl]-2-(4-hydroxyphenyl)-3-methyl-1H-indol-5-ol acetic acid, and has the chemical structure shown below as Formula I. | 08-29-2013 |
| 20160107991 | PROCESSES AND INTERMEDIATES FOR PREPARING INDOLE PHARMACEUTICALS - The invention described herein pertains to processes and intermediates for preparing indole containing pharmaceuticals, particularly to processes and intermediates for preparing selective estrogen receptor modulators, such as bazedoxifene. | 04-21-2016 |
| 540603000 | Plural hetero atoms in the additional hetero ring | 4 |
| 20090216013 | Heteroaryl-Ureas and Their Use as Glucokinase Activators - This invention relates to compounds of formula (I) | 08-27-2009 |
| 20100048891 | METASUBSTITUTED THIAZOLIDINONES, THEIR MANUFACTURE AND USE AS A DRUG - Thiazolidinones of general formula (I) | 02-25-2010 |
| 20100105896 | PHARMACEUTICAL COMPOUNDS - Pyrazole derivatives of the following formula (I), having affinity for the cannabinoidergic CB1 and/or CB2 receptors: | 04-29-2010 |
| 20110213145 | Compounds and Methods for Inhibiting the Interaction of BCL Proteins with Binding Partners - The invention relates to isoxazolidine containing compounds that bind to bcl proteins and inhibit Bcl function. The compounds may be used for treating and modulating disorders associated with hyperproliferation, such as cancer. | 09-01-2011 |
