Class / Patent application number | Description | Number of patent applications / Date published |
546195000 | The additional ring is one of the cyclos in a polycyclo ring system | 76 |
546196000 | Hetero ring in the polycyclo ring system | 61 |
20100004456 | Oxepin derivative - The present invention provides a compound, an oxepin derivative having excellent histamine receptor antagonistic action, which is useful as an antihistamine. The oxepin derivative of the present invention has a potent histamine receptor antagonistic action. Further, the compound of the present invention shows low intracerebral migration even when a mouse that is orally administered with the compound is subjected to an intracerebral receptor binding test, so that the compound has preferred properties of alleviating side effects in the central nervous system, such as drowsiness. The oxepin derivative of the present invention is very useful as a novel antihistamine having smaller side effects in the central nervous system, such as drowsiness. | 01-07-2010 |
20100113792 | BENZYLPIPERIZINE COMPOUND - Disclosed is a benzylpiperizine compound represented by formula (1) or a pharmaceutically acceptable salt thereof, which is useful as a medicinal agent such as an antidepressant agent. (In the formula (1), R | 05-06-2010 |
20100324296 | DICHROIC-PHOTOCHROMIC COMPOUNDS AND DEVICES - A naphthopyran compound represented by the formula | 12-23-2010 |
20120130077 | BENZYL PIPERIDINE COMPOUND - Provided is a new serotonin-reuptake inhibitor that exhibits affinity for serotonin-1A receptors. Said serotonin-reuptake inhibitor is a compound represented by formula (1) or a pharmacologically acceptable salt thereof. In the formula, R | 05-24-2012 |
20120209005 | FUSED HETEROCYCLIC COMPOUNDS AND THROMBOPOIETIN RECEPTOR ACTIVATORS - Fused heterocyclic compounds useful for prevention, treatment or improvement of diseases against which activation of the thrombopoietin receptor is effective are provided. | 08-16-2012 |
20130331578 | NOVEL IMINOSUGARS AND THEIR APPLICATIONS - Iminosugar compounds are described that have inbuilt delivery features by virtue of covalent incorporation of a tocopherol moiety, or alternative moieties that are analogues of tocopherol or select analogues of cholesterol, or its antagonist “Ezitimibe”; and are likely to have broad spectrum antiviral activity. The compounds differ from previous iminosugar compounds, even lipophillic ones, being more hydrophobic and resembling fats and oils in their partition behavior in vivo into lipid phases of lipoproteins, cellular lipid droplet organelles and biological membranes. These features confer a number of unique delivery attributes in vivo, favorable to the therapy of virus infections involving cells of the lymphoid system and the liver, in particular, but these features are also favorable in general for the treatment of virus infections of man and animals. | 12-12-2013 |
20160046611 | NOVEL CHROMONE ALKALOID DYSOLINE FOR THE TREATMENT OF CANCER AND INFLAMMATORY DISORDERS - The present invention relates to novel chromone alkaloid of formula 1 isolated from the plant | 02-18-2016 |
546197000 | Plural ring hetero atoms in the polycyclo ring system | 20 |
20100222589 | DEUTERATED BENZO[D][1,3]-DIOXOL DERIVATIVES - The present invention relates to an isotopologue of Compound 1 substituted with deuterium at the methylene carbon of the benzodioxol ring. The isotopologues of this invention selective serotonin reuptake inhibitors (SSRIs) and possess unique biopharmaceutical and metabolic properties compared to Compound 1. They may also be used to accurately determine the concentration of Compound 1 in biological fluids and to determine metabolic patterns of Compound 1 and its isotopologues. The invention further provides compositions comprising these deuterated isotopologues and methods of treating diseases and conditions that are responsive to increased neuronal serotonin transmission, alone and in combination with additional agents. | 09-02-2010 |
20140179926 | 2,3-DIHYDROBENZO[1,4] DIOXIN-2-YLMETHYL DERIVATIVES AS ALPHA2C ANTAGONISTS FOR USE IN THE TREATMENT OF PERIPHERIC AND CENTRAL NERVOUS SYSTEM DISEASES - Compounds of formula I | 06-26-2014 |
20140336387 | SYNTHESIS OF DEUTERATED CATECHOLS AND BENZO[D][1,3]DIOXOLES AND DERIVATIVES THEREOF - The present invention provides a convenient and efficient process for the synthesis of d | 11-13-2014 |
20160200720 | HETEROARYLPIPERIDINE AND PIPERAZINE DERIVATIVES AS FUNGICIDES | 07-14-2016 |
546198000 | Ring nitrogen in the polycyclo ring system | 16 |
20100076196 | PROCESS FOR THE PREPARATION OF ILOPERIDONE - A process for the preparation of crystalline 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]propoxy]-3-methoxyphenyl]-ethanone (Iloperidone), which comprises the reaction between 3-[1-(3-chloropropyl)-4-piperidinyl]-6-fluoro-1,2-benzisoxazole and 3-methoxy-4-hydroxy-acetophenone. | 03-25-2010 |
20110034694 | COMPOUNDS HAVING BETA2 ADRENERGIC RECEPTOR AGONIST AND MUSCARINIC RECEPTOR ANTAGONIST ACTIVITY - The invention is directed to compounds of formula I: | 02-10-2011 |
20120065403 | Benzothiazole Derivatives - Provided are compounds and their pharmaceutically acceptable salts that are useful for the treatment of diseases related to the adenosine receptor. Also included are methods of treating patients suffering from or susceptible to at least one symptom of abuse of, dependence on, or withdrawal from at least one substance. | 03-15-2012 |
20120172600 | METHOD FOR PREPARATION OF ILOPERIDONE AND CRYSTALLIZATION METHOD THEREOF - A method for preparation of iloperidone is provided which comprises reacting 6-fluoro-3-(4-piperidinyl)-1,2-benzoisoxazole hydrochloride with 1-[4-(3-chloropropoxyl)-3-methoxyphenyl]ethyl ketone in an inorganic alkaline aqueous solution. A crystallization method of iloperidone is also provided which comprises adding seed crystal to the iloperidone solution in ethyl acetate, and then iloperidone crystal is obtained with high purity by controlling the temperature and the stirring speed. | 07-05-2012 |
20120220776 | PROCESS FOR THE PREPARATION OF ILOPERIDONE USING A NOVEL INTERMEDIATE - The present invention provides a novel process for the preparation of iloperidone using a novel intermediate. Thus, for example, 4-(3-chloropropoxy)-3-methoxybenzaldehyde is reacted with methyl magnesium iodide in ether and the reaction mass is heated for 6 hours at reflux temperature, the resulting mass is cooled to ambient temperature and then poured into a mixture of ice, water and dilute hydrochloric acid to produce 1-[4-(3-chloropropoxy)-3-methoxyphenyl]ethanol, which is then subsequently converted to iloperidone. | 08-30-2012 |
20130190501 | PROCESSES FOR THE PREPARATION OF 4'-[3-[4-(6-FLUORO-1,2-BENZISOXAZOL-3-YL)PIPERIDINO]PROPOXY]-3'-METHOXYAC- ETOPHENONE AND INTERMEDIATES THEREOF - The present invention relates to processes for the preparation of 4′-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino]propoxy]-3′-methoxyacetophenone and intermediates thereof. The present invention also provides a process for purifying 4′-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidino]propoxy]-3′-methoxyacetophenone to obtain the purity greater than about 98.0 area % to about 99.0 area % as measured by HPLC, preferably greater than about 99.0 area % to about 99.5 area %, more preferably greater about 99.5 area % to about 99.9 area %. individual impurities lower than about 0.15 area %, preferably lower than about 0.1% and total impurities lower than about 0.5 area % by HPLC. | 07-25-2013 |
20130261308 | ONE-POT PROCESS FOR THE SYNTHESIS OF ILOPERIDONE - Disclosed is a process for the synthesis of iloperidone starting from 4-hydroxy-3-methoxy acetophenone (acetovanillone), 1-chloro-3-bromo propane and 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole hydrochloride, using a one-pot method. | 10-03-2013 |
20140179927 | METHOD FOR PREPARATION OF ILOPERIDONE AND CRYSTALLIZATION METHOD THEREOF - A method for preparation of iloperidone is provided which comprises reacting 6-fluoro-3-(4-piperidinyl)-1,2-benzoisoxazole hydrochloride with 1-[4-(3-chloropropoxyl)-3-methoxyphenyl]ethyl ketone in an inorganic alkaline aqueous solution. A crystallization method of iloperidone is also provided which comprises adding seed crystal to the iloperidone solution in ethyl acetate, and then iloperidone crystal is obtained with high purity by controlling the temperature and the stirring speed. | 06-26-2014 |
546199000 | Plural ring nitrogens in the polycyclo ring system | 8 |
20100048907 | INDAZOLAMIDES WITH ANALGESIC ACTIVITY - The present invention relates to compounds of formula (II) | 02-25-2010 |
20100217005 | EPOXY COMPOUND AND METHOD FOR MANUFACTURING THE SAME - The present invention provides a novel intermediate for manufacturing a 2,3-dihydroimidazo[2,1-b]oxazole compound with a high yield and a high purity, and a manufacturing method of the intermediate. The present invention provides an epoxy compound represented by the general formula (2): wherein, R1 represents hydrogen or a lower alkyl group; and R2 represents a piperidyl group represented by the general formula (A1): (wherein, R3 represents a phenoxy group having a halogen-substituted lower alkoxy group substituted on a phenyl group, and the like) and the like; and n represents an integer of 1 to 6, a manufacturing method of the epoxy compound, and a manufacturing method of an oxazole compound using the epoxy compound. | 08-26-2010 |
20110009636 | PROCESS FOR THE PREPARATION OF 2-METHYL-2'-PHENYLPROPIONIC ACID DERIVATIVES AND NOVEL INTERMEDIATE COMPOUNDS - The present invention relates to a process for preparing 2-methyl-2′-phenylpropionic acid derivatives showing antihistamine activity in more simplified way, intermediate compounds and their preparation processes used therefor. According to the present invention, pharmaceutically useful 2-methyl-2′-phenylpropionic acid derivatives can be prepared with high yield and purity on industrial scale. | 01-13-2011 |
20110282066 | SCREENING METHOD FOR SUBSTANCE USEFUL AS AGENT FOR TREATING PROSTATE CANCER - [Object] A screening method for a compound which is useful as an agent for treating 17βHSD type 5-related diseases and/or an agent for treating 17βHSD type 5-related cancer such as prostate cancer is provided. | 11-17-2011 |
20110295013 | PROCESS FOR PREPARING 1-(4-PIPERIDINYL)BENZIMIDAZOLONE DERIVATIVES - Provision of an industrial method of producing a 1-(4-piperidinyl)benzimidazolone derivative in a high yield at a low cost. | 12-01-2011 |
20120130078 | INDAZOLE DERIVATIVES AS ADENOSINE MONOPHOSPHATE DEAMINASE (AMPD) INHIBITORS FOR USE IN DIABETES AND RELATED DISEASES OF METABOLIC SYNDROME - Herein, we describe a method for treatment of diabetes and other disorders classified as Metabolic Syndrome. The invention provides novel AMP Deaminase (AMPD) inhibitors comprising novel indazole and benzotriazole derivatives including a phosphorous containing derivative, a carboxylic acid, or an amino acid ester prodrug. The invention also provides support for a novel mechanism of action for the existing drug metformin: direct inhibition of the enzyme AMPD. The inhibition of AMPD in turn activates AMP Kinase, known to be linked to the action of metformin. The invention also makes novel use of a double inhibitor assay allowing identification of selective AMPD inhibitors over ADA inhibitors. The new inhibitors, structurally distinct from metformin, offer selectivity that may obviate side effects known for metformin itself, providing new benefits for diabetes and Metabolic Syndrome. | 05-24-2012 |
20130116439 | PROCESS FOR PREPARATION OF 2-METHYL-2'-PHENYLPROPIONIC ACID DERIVATIVES AND NOVEL INTERMEDIATE COMPOUNDS - The present invention relates to a process for preparing 2-methyl-2′-phenylpropionic acid derivatives showing antihistamine activity in more simplified way, intermediate compounds and their preparation processes used therefore. According to the present invention, pharmaceutically useful 2-methyl-2′-phenylpropionic acid derivatives can be prepared with high yield and purity on industrial scale. | 05-09-2013 |
20150299167 | Regioselective N-2 Arylation of Indazoles - A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: | 10-22-2015 |
546200000 | Ring nitrogen in the polycyclo ring system | 31 |
20090171093 | 3'-Fluoro-5'-hydroxythalidomide and derivatives thereof - There are provided a novel 3′-fluoro-5′-hydroxythalidomide derivative and an optically active substance thereof A 3′-fluoro-5′-hydroxythalidomide derivative represented by the general formula [A]: | 07-02-2009 |
20090187023 | POLYMORPHIC FORMS OF 3-(4-AMINO-1-OXO-1,3 DIHYDRO-ISOINDOL-2-YL))-PIPERIDINE-2,6-DIONE - Polymorphic forms of 3-(4-amino-1-oxo-1,3 dihydro-isoindol-2-yl)-piperidine-2,6-dione are disclosed. Compositions comprising the polymorphic forms, methods of making the polymorphic forms and methods of their use are also disclosed. | 07-23-2009 |
20090192314 | PROCESS FOR THE PREPARATION OF CHIRAL 8-(3-AMINOPIPERIDIN-1YL)-XANTHINES - The invention relates to an improved process for preparing enantiomerically pure 8-(3-aminopiperidin-1-yl)-xanthines. | 07-30-2009 |
20100280249 | SYNTHESIS OF 4-AMINO-THALIDOMIDE ENANTIOMERS - The invention provides new and useful analogs of 4-amino-thalidomide. These analogs include S(−)-4-amino-thalidomide and R(+)-4-amino-thalidomide. The invention also provides processes for making these analogs. Further, the invention provides methods for inhibiting angiogenesis and treating angiogenesis-associated diseases, including cancer and macular degeneration, by administering these compounds. | 11-04-2010 |
20110224440 | PROCESSES FOR THE PREPARATION OF 4-AMINO-2-(2,6-DIOXOPIPERIDIN-3-YL)ISOINDOLINE-1,3-DIONE COMPOUNDS - The present invention provides new processes for the preparation of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds which are useful, for example, for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-α. The invention can provide improved and/or efficient processes for the commercial production of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds, including, but not limited to, unsubstituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione. | 09-15-2011 |
20120165536 | 4'-O-SUBSTITUTED ISOINDOLINE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME - Provided are 4′-O substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed. | 06-28-2012 |
20120184746 | PROCESS FOR THE PREPARATION OF LENALIDOMIDE - The present invention relates to a process for the preparation of lenalidomide, wherein the process comprises: reducing 3-(4-nitro-loxo-1,3-dihydro-2H-isoindol-2-yl)piperidine-2,6-dione to obtain lenalidomide. | 07-19-2012 |
20120220777 | PROCESS FOR THE PREPARATION OF A CRYSTALLINE FORM OF LENALIDOMIDE - The present invention relates to an in-situ process for the preparation of polymorphic Form A of lenalidomide. | 08-30-2012 |
20140256950 | PROCESSES FOR THE PREPARATION OF 4-AMINO-2-(2,6-DIOXOPIPERIDIN-3-YL)ISOINDOLINE-1,3-DIONE COMPOUNDS - The present invention provides new processes for the preparation of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds which are useful, for example, for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-α. The invention can provide improved and/or efficient processes for the commercial production of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds, including, but not limited to, unsubstituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione. | 09-11-2014 |
20140364615 | INDOLE DERIVATIVES - An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent. | 12-11-2014 |
20150094473 | SOLID FORMS OF 3-(4-NITRO-1-OXOISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE - Solid forms comprising crystalline 3-(4-nitro-1-oxoisoindolin-2-yl)piperidine-2,6-dione are disclosed. Compositions comprising the solid forms, methods of making the solid forms and methods of their use are also disclosed. | 04-02-2015 |
20150141652 | PROCESS FOR PREPARING 2-[(2E)-2-FLUORO-2-(3-PIPERIDINYLIDENE)ETHYL]-1H-ISOINDOLE-1,3(2H)-DIONE - The present invention relates to an improved process for preparing 2-[(2E)-2-fluoro-2-(3-piperidinylidene)ethyl]-1H-isoindole-1,3(2H)-dione, or a salt thereof, which is an intermediate in the synthesis route of the antibacterial compound 7-[(3E)-3-(2-amino-1-fluoroethylidene)-1-piperidinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-4-oxo 3-quinolinecarboxylic acid. | 05-21-2015 |
20150299162 | SOLID FORMS OF - The invention in one embodiment is directed to solid forms of {S-3-(4-Amino-1-oxo-isoindolin-2-yl)(piperidine-3,4,4,5,5-d | 10-22-2015 |
546201000 | Bicyclo ring system which is indole (including hydrogenated) | 18 |
20090069565 | NEW INDOLE DERIVATIVES AS FACTOR XA INHIBITORS - The present invention relates to compounds of formula I, | 03-12-2009 |
20090264656 | METHOD FOR MANUFACTURE OF SERTINDOLE - The present invention relates to a novel method for manufacture of sertindole comprising manufacturing 5-chloro-1-(4-fluorophenyl)-indole and converting it to sertindole wherein the method for manufacture of 5-chloro-1-(4-fluorophenyl)-indole comprises reacting 5-chloro-indole with a 4-fluorophenylhalide in the presence of a base, a chelating ligand and catalytic amounts or a copper salt comprising copper(I) or copper(II) and an anion which does not interfere in an unfavourable way with the reaction. | 10-22-2009 |
20090286986 | ISOINDOLE-IMIDE COMPOUNDS, COMPOSITIONS, AND USES THEREOF - The invention relates to isoindole-imide compounds and pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions comprising these isoindole-imide compounds, and methods for reducing the level of cytokines and their precursors in mammals. In particular, the invention pertains to isoindole-imide compounds that are potent inhibitors of the production of TNF-α in mammals. The isoindole-imides described herein are useful for treating or preventing diseases or disorders in mammals, for example, cancers, such as solid tumors and blood-born tumors; heart disease, such as congestive heart failure; osteoporosis; and genetic, inflammatory; allergic; and autoimmune diseases. | 11-19-2009 |
20100197926 | METHOD FOR PRODUCING INDOLE DERIVATIVE HAVING PIPERIDINE RING - It is possible to commercially advantageously prepare 1-{1-[2-(7-methoxy-2,2-dimethyl-4-oxochroman-8-y)ethyl]piperidin-4-yl}-N-methyl-1H-indole-6-carboxamide by coupling (7-methoxy-2,2-dimethyl-4-oxochroman-8-yl)acetaldehyde, which is obtained by oxidizing 8-(2-hydroxyethyl)-7-methoxy-2,2-dimethylchroman-4-one, with N-methyl-1-(piperidin-4-yl)-1H-indole-6-carboxamide. | 08-05-2010 |
20110003996 | Crystal Forms of (3R)-1-(2-Methylalanyl-D-Tryptophyl)-3-(Phenylmethyl)-3-Piperidinecarboxy- lic Acid 1,2,2-Trimethylhydrazide - Crystalline polymorphs of (3R)-1-(2-methylalanyl-D-tryptophyl)-3-(phenylmethyl)-3-piperidinecarboxylic acid 1,2,2-trimethylhydrazide which are useful as pharmaceutical agents are disclosed. Methods of production and isolation of these polymorphs and pharmaceutical compositions which include these polymorphs and pharmaceutical methods of treatment are also disclosed. The crystalline polymorphs of the present invention are useful as they act directly on the pituitary gland cells to release growth hormone. | 01-06-2011 |
20110105758 | PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY ENRICHED CYCLIC BETA-ARYL OR HETEROARYLCARBOCYCLIC ACIDS - The present invention relates to a process for the preparation of cis substituted cyclic β-aryl or heteroaryl carboxylic acid derivatives in high diastereo- and enantioselectivity by enantioselective hydrogenation in accordance with the following scheme | 05-05-2011 |
20120077982 | Methods for Synthesizing 3-(Substituted Dihydroisoindolinone-2-YL)-2, 6-Dioxopiperidine, and Intermediates Thereof - The present invention discloses methods for synthesizing 3-(substituted dihydroisoindolinone-2-yl)-2,6-dioxopiperidine and intermediates thereof, namely, the synthesis of compounds of the Formula (I), with each substitutional group defined in the patent specification. Owing to the advantages of high productivity, little influence to the environment and material accessibility, the methods of the present invention is suitable for industrial production. | 03-29-2012 |
20120203005 | POLYMORPH OF 3-(SUBSTITUTEDDIHYDROISOINDOLINONE-2-YL)-2,6-DIOXOPIPERIDINE, AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention provides polymorph of 3-(4-amino-1-oxo-1,3-dihydro-2H-isoindole-2-yl)-piperidine-2,6-dione, and also the preparing methods and pharmaceutical compositions thereof. | 08-09-2012 |
20120220778 | Process for the synthesis of naratriptan - The present invention relates to a process for preparing naratriptan or a salt thereof, the process comprising: (a) reacting a compound of formula (3) with a compound of the formula HCCR | 08-30-2012 |
20120245357 | ALR2 INHIBITORS AND THEIR SYNTHESIS FROM A NATURAL SOURCE - A Michael adduct of piplartine, to provide inhibition of ALR2 in vitro (supported by molecular docking) and their potential to suppress the accumulation of sorbitol in erythrocytes when incubated under high glucose conditions; a treatment method using a Michael adduct; and a process for preparing a Michael adduct are provided. | 09-27-2012 |
20130172563 | LENALIDOMIDE SOLVATES AND PROCESSES - The present application relates to lenalidomide salts and solvates, and processes for the preparation thereof. | 07-04-2013 |
20130253201 | PROCESS FOR THE PREPARATION OF ENANTIOMERICALLY ENRICHED CYCLIC BETA-ARYL OR HETEROARYL CARBOCYCLIC ACIDS - The present invention relates to a process for the preparation of cis substituted cyclic β-aryl or heteroaryl carboxylic acid derivatives in high diastereo- and enantioselectivity by enantioselective hydrogenation in accordance with the following scheme | 09-26-2013 |
20130281701 | CRYSTAL FORMS OF ANAMORELIN - Crystalline forms of anamorelin which are useful as pharmaceutical agents are disclosed. Methods of production and isolation of these polymorphs and pharmaceutical compositions which include these polymorphs and pharmaceutical methods of treatment are also disclosed. The crystalline polymorphs of the present invention are useful as they act directly on the pituitary gland cells to release growth hormone. | 10-24-2013 |
20140031552 | PROCESSES FOR PREPARING ISOINDOLINE-1,3-DIONE COMPOUNDS - Provided herein are processes for preparing an isoindoline-1,3-dione compound, or an enantiomer or a mixture of enantiomers thereof; or a pharmaceutically acceptable salt, solvate, hydrate, or polymorph thereof. | 01-30-2014 |
20150353489 | Erythropoietin Expression Promoter - The present invention provides an erythropoietin expression-enhancing agent that can cancel the suppression of erythropoietin production or promote erythropoietin production, and a therapeutic or preventive drug for anemia, a liver function-improving agent, an ischemic injury-improving agent, a renal protective agent, and an insulin secretagogue comprising the erythropoietin expression-enhancing agent. The erythropoietin expression-enhancing agent of the present invention comprises one or more compounds selected from the group consisting of compounds represented by the following general formulas (I), (II), and (III) and pharmaceutically acceptable salts thereof when R | 12-10-2015 |
20150353525 | ANHYDROUS LENALIDOMIDE FORM-I - Anhydrous polymorphic form-I of anti cancer drug, Lenalidomide whose chemical name is 3-(4-amino-1-oxo-1,3-dihydro-isoindole-2-yl)-piperidine-2,6-dione, is disclosed. Alternate methods for making anhydrous polymorphic form-I of Lenalidomide are also disclosed. | 12-10-2015 |
20160009684 | POLYMORPHIC FORMS OF 3-(4-AMINO-1-OXO-1,3 DIHYDRO-ISOINDOL-2-YL)-PIPERIDINE-2,6-DIONE | 01-14-2016 |
20160046667 | Crystal Forms of Anamorelin - Crystalline forms of anamorelin which are useful as pharmaceutical agents are disclosed. Methods of production and isolation of these polymorphs and pharmaceutical compositions which include these polymorphs and pharmaceutical methods of treatment are also disclosed. The crystalline polymorphs of the present invention are useful as they act directly on the pituitary gland cells to release growth hormone. | 02-18-2016 |
546202000 | Ring sulfur in the polycyclo ring system | 3 |
20090111992 | ALKYL ETHER DERIVATIVES OR SALTS THEREOF - An alkyl ether derivative represented by the general formula: | 04-30-2009 |
20100137602 | PROCESS AND INTERMEDIATES FOR PREPARING ARZOXIFENE - The present invention provides for novel compounds of formula I wherein X is S or S(O); R | 06-03-2010 |
20120123127 | PROCESS FOR PRODUCING THIABENZOAZULENE-PROPIONIC ACID DERIVATIVE - Disclosed is a process for producing a thiabenzoazulene-propionic acid derivative which is useful as an active ingredient of an antihistaminic agent or the like. According to the producing process of the present invention, it is possible to produce a thiabenzoazulene-propionic acid derivative where the 2-position of the thiabenzoazulene skeleton is substituted with propionic acid. The thiabenzoazulene propionic-acid derivative thus synthesized has excellent antagonistic action to histamine H1 receptor and low intracerebral transmigration and, therefore, is useful as an active ingredient of the pharmaceutical composition such as an antihistaminic agent. | 05-17-2012 |
546203000 | The polycyclo ring system is tricyclo-carbocyclic | 2 |
20080207908 | PROCESSES FOR THE PREPARATION OF PIPERIDINYL-SUBSTITUTED UREA COMPOUNDS - Disclosed are processes for the synthesis of piperidinyl-substituted urea compounds. This invention further relates to novel intermediates prepared during this synthesis. | 08-28-2008 |
546204000 | Chalcogen bonded directly to the tricyclo-carbocyclic ring system | 1 |
20130053571 | PLEUROMUTILINS AND PROCESS FOR THE PREPARATION OF PLEUROMUTILINS - A process for the preparation of 14-O—[(N-(3-methyl-2-amino-butyryl-piperidinyl)sulfanyl)acetyl]mutilins of formula | 02-28-2013 |
546205000 | The polycyclo ring system is bicyclo-carbocyclic | 13 |
20080234485 | 1-Benzyl-4-[ (5,6-Dimethoxy-1-Indanon) -2-Yl] Methylpiperidine Hydrobromide or Crystals Thereof - 1-Benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine hydrobromide or a solvate thereof. | 09-25-2008 |
20100081825 | 1-NAPHTHYL ALKYLPIPERIDINE DERIVATIVE - Disclosed is a pharmaceutical composition comprising a compound represented by the formula (I) | 04-01-2010 |
546206000 | Chalcogen bonded directly to the bicyclo-carbocyclic ring system | 11 |
20080306271 | Novel Process for Production of Highly Pure Polymorph (I) Donepezil Hydrochloride - The present invention provides a novel, industrially realizable and economically preferable process for production of highly pure 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methyl piperidine hydrochloride, i.e., donepezil hydrochloride shown in the following reaction scheme, in Polymorph (I) morphological crystal form. (I) In one of the key steps of the process, during the hydrogenation 5,6-dimethoxy 2-(pyridine-4-yhnethylene)indan- | 12-11-2008 |
20090137812 | PROCESS FOR PRODUCING 1-BENZYL-4-[5,6-DIMETHOXY-1-INDANON-2-YL)METHYL]PIPERIDINE OR ITS SALT THEREOF VIA NOVEL INTERMEDIATE - Disclosed herein the process for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon-2yl)methyl]piperidine or its salt thereof employing novel intermediates. | 05-28-2009 |
20090171094 | 1-BENZYL-4-[(5, 6-DIMETHOXY- 1- INDANON)- 2- YL]-METHYL PIPERIDINE P-TOLUENESULFONATE OR CRYSTAL THEREOF - 1-Benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methylpiperidine p-toluenesulfonate or a solvate thereof. | 07-02-2009 |
20100105916 | Processes for Preparing Donepezil - A process for preparing highly pure donepezil, particularly donepezil hydrochloride, is provided comprising hydrogenating compound 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-ylidene]methyl-piperidine or its hydrochloride salt with a noble metal catalyst or a derivative thereof, in the presence of at least one additive, wherein the additive contains at least one heteroatom, e.g., a sulfur, phosphorous, or nitrogen heteroatom. | 04-29-2010 |
20100113793 | Process for the Preparation of Highly Pure Donepezil - The present invention relates to the preparation of highly pure donepezil of formula I or salt thereof, by hydrogenating indanonylidenyl compound of formula II, using platinum catalysts. | 05-06-2010 |
20110105759 | PROCESS FOR PRODUCING 1-BENZYL-4- [ (5,6-DIMETHOXY-1-INDANONE)-2-YLIDENE] METHYLPIPERIDINE - It is intended to provide a process for producing 1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-ylidene]methylpiperidine represented by the structural formula (I): (I) which is useful as an intermediate material for a pharmaceutical or a solvate thereof in which impurity content is further reduced and operation is simple and suitable for industrial production by reacting 5,6-dimethoxy-1-indanone with 1-benzyl-4-formylpiperidine in a reaction solvent in the presence of a base and then gradually crystallizing a target substance in a reaction mixture in a high temperature region. | 05-05-2011 |
20110230663 | PROCESS FOR THE PREPARATION OF DONEPEZIL HYDROCHLORIDE - The present invention relates to novel process for preparing Donepezil hydrochloride of formula (I) | 09-22-2011 |
20120323012 | 4-(AZACYCLOALKYL) -BENZENE-1,3-DIOL DERIVATIVES AS TYROSINASE INHIBITORS AND THEIR SYNTHESIS AND USE THEREOF - 4-(azacycloalkyl)-benzene-1,3-diol compounds with the following general formula (I): | 12-20-2012 |
20130035490 | Method For Making Donepezil - The method in accordance with the present invention has: mixing E2M, an organic solvent, a weak base, sodium dithionite, and a phase transfer catalyst to obtain an E2M mixture solution; heating the E2M mixture solution and adding water to obtain a heated E2M aqueous solution having an organic layer; and extracting the organic layer from the heated E2M aqueous solution, and condensing and drying the organic layer to obtain donepezil. Employing sodium dithionite as a reducing agent improves safety over hydrogen gas used in conventional methods and lowers the cost in contrast to the conventional noble metal catalysts that are extremely expensive. Furthermore, the method of the present invention requires only 60 minutes of reaction time to synthesize donepezil with a promising yield more than 85%, which greatly raises the efficiency and economic value of the manufacture of donepezil. | 02-07-2013 |
20160008335 | PHARMACEUTICAL COMPOSITIONS OF DONEPEZIL HAVING SPECIFIC IN VITRO DISSOLUTION PROFILE OR PHARMACOKINETICS PARAMETERS | 01-14-2016 |
20160015698 | PHARMACEUTICAL COMPOSITIONS OF DONEPEZIL HAVING SPECIFIC IN VITRO DISSOLUTION PROFILE OR PHARMACOKINETICS PARAMETERS - A timed release pharmaceutical composition comprising donepezil is provided wherein the single dose AUC(14-22) of the said composition administered in the morning is about % to about 30% less than the single dose AUC(2-10) of an immediate release composition of donepezil administered in the night, wherein both the compositions have equivalent dose of donepezil. | 01-21-2016 |