Class / Patent application number | Description | Number of patent applications / Date published |
546118000 | Three ring nitrogens in the bicyclo ring system | 38 |
20090176986 | Process for the Preparation of Pyridine Heterocycle Cgrp Antagonist Intermediate - An efficient syntheses for the preparation of the intermediate 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine dihydrochloride, and other salt forms of 2-oxo-1-(4-piperidinyl)-2,3-dihydro-1H-imidazo[4,5-b]pyridine. | 07-09-2009 |
20090203912 | Regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles - The present invention relates to a process for the regioselective synthesis of compounds of the formula I, | 08-13-2009 |
20090306388 | METHOD FOR SUBSTITUTED IH-IMIDAZO[4,5-C] PYRIDINES - Methods for preparing compounds of the Formulas IV and I are disclosed. The methods include combining a compound of the Formula II: with a benzylamine of the Formula III: in the presence of an acid to provide a 1H-imidazo[4,5-c]pyridine compound of the Formula IV. | 12-10-2009 |
20100145054 | IMIDAZOLE DERIVATIVES HAVING ARYL PIPERIDINE SUBSTITUENT, METHOD FOR PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME - The present invention is directed to a novel imidazole derivative having an aryl piperidine substituent of formula (I) and a method for preparation thereof, and a pharmaceutical composition containing said imidazole derivative as an active ingredient for preventing or treating a MCH (melanine-concentrating hormone)-related disease. | 06-10-2010 |
20100217000 | Process for the Preparation of Thiazolopyrimidines - A method for the preparation of a compound of formula (1) or a pharmaceutically acceptable salt or solvate thereof; from a compound of the formula: (IV); wherein L represents a leaving group. | 08-26-2010 |
20100234601 | Transition metal catalyzed synthesis of 2H-indazoles - The present invention relates to a process for the regioselective synthesis of compounds of the formula I, | 09-16-2010 |
20100261909 | Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles - The present invention relates to a process for the regioselective synthesis of compounds of the formula I, | 10-14-2010 |
20100305324 | PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING OSTEOPOROSIS OR OBESITY COMPRISING PHENYLTETRAZOLE DERIVATIVE - A phamaceutical composition comprising a phenyltetrazole derivative of formula (I) or a pharmaceutical acceptable salt thereof is effective in preventing or treating osteoporosis, obesity, diabetes, or hyperlipidemia, by regulating protein TAZ. | 12-02-2010 |
20120203003 | Continuous Flow Process For The Preparation Of Sulphoxide Compounds - A continuous micromixer based process for the synthesis of sulphoxide compounds with a reaction time of less than or equal one minute is disclosed. The process shows selectivity of >95% towards the sulphoxide compounds. | 08-09-2012 |
20120245356 | Process for the Preparation of Cycloheptapyridine CGRP Receptor Antagonists - The disclosure generally relates to a process for the preparation of compounds of formula I, including synthetic intermediates which are useful in the process. | 09-27-2012 |
20130053570 | CGRP Receptor Antagonists - The disclosure generally relates to the novel compounds of formula I, including pharmaceutically acceptable salts, which are CGRP receptor antagonists. The disclosure also relates to pharmaceutical compositions and methods for using the compounds in the treatment of CGRP related disorders including migraine and other headaches, neurogenic vasodilation, neurogenic inflammation, thermal injury, circulatory shock, flushing associated with menopause, airway inflammatory diseases such as asthma, and chronic obstructive pulmonary disease (COPD). | 02-28-2013 |
20130267711 | TRICYCLIC COMPOUND - The invention provides a method of activating PPAR γ and a method of treating or preventing a disease associated with PPAR γ by administering a tricyclic compound having a PPAR γ agonist activity, which is represented by the formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R | 10-10-2013 |
20140206874 | CRYSTAL FORM I OF SALT OF A DIPEPTIDYL PEPTIDASE-IV INHIBITOR AND PREPARATION METHOD AND USE SAME - The present invention relates to the crystal form I of salt of a dipeptidyl peptidase-IV inhibitor, and the preparation method and use thereof. In particular, it relates to the crystal form I of dihydrochloride salt of the compound (R)-2-[[7-(3-aminopiperidin-1-yl)-3,5-dimethyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl]methyl]benzonitrile represented by formula (1), which is a dipeptidyl peptidase-IV inhibitor, and the preparation method and use thereof. The crystal form I of dihydrochloride salt of the dipeptidyl peptidase-IV inhibitor represented by formula (1) is characterized in that it has characteristic peaks at 8.7±0.2°, 19.4±0.2°, 23.5±0.2° and 27.2±0.2° in X-ray powder diffraction indicated by an angle 2θ (°) using Cu-Kα irradiation. | 07-24-2014 |
20150291587 | TRICYCLIC COMPOUND - The invention provides a method of activating PPAR γ and a method of treating or preventing a disease associated with PPAR γ by administering a tricyclic compound having a PPAR γ agonist activity, which is represented by the formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R | 10-15-2015 |
20150322065 | Azabenzimidazole Compounds - The present invention is directed to compounds of formula I: | 11-12-2015 |
20160376270 | PROCESS OF PREPARING 3-(3-(4-(1-AMINOCYCLOBUTYL)PHENYL)-5-PHENYL-3H-IMIDAZO[4,5-B]PYRIDIN-2-YL- )PYRIDIN-2-AMINE - The present invention is directed to a processes for the synthesis of 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine: | 12-29-2016 |
546119000 | Two of the ring nitrogens are bonded directly to each other | 22 |
20090012299 | Pyrazolo-pyridinone compounds and methods of use thereof - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula I | 01-08-2009 |
20090076275 | DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS - Provided herein are compounds of the formula (I): | 03-19-2009 |
20100168430 | MULTIKINASE INHIBITOR - It is intended to provide a compound represented by the formula (1): | 07-01-2010 |
20110172427 | PROCESS FOR PREPARING CERTAIN CINNAMIDE COMPOUNDS - This invention relates to a new synthesis, intermediates and precursors leading to a mixture of the compounds 11 and 12 as shown below. It also relates to the resolution of the stereoisomeric mixture to provide in substantial stereochemical purity compound 12. The synthesis of the invention involves preparation of compound 7 and compound 10 as shown below and their reaction to prepare a mixture of compound 11 and compound 12. | 07-14-2011 |
20110257402 | PYRRAZOLOPYRIDINE COMPOUNDS AS DUAL NK1/NK3 RECEPTOR ANTAGONISTS - The present invention relates to a compound of formula I | 10-20-2011 |
20110275822 | SALT OF TETRAHYDROTRIAZOLOPYRIDINE DERIVATIVE AND CRYSTAL THEREOF - The present invention provides a crystal of a 1.5 D-tartrate of a compound represented by the formula (1) having an A production inhibitory effect, characterized in that the crystal has a diffraction peak at a diffraction angle (20.2) of 23.2 in powder X-ray diffractometry; a crystal of a disulfate of the compound of the formula (1), characterized in that the crystal has a diffraction peak at a diffraction angle (20.2) of 17.1 in powder X-ray diffractometry; various other salts of the compound of the formula (1); crystal polymorphs of these salts; and the like, which are expected to be used as drug substances. | 11-10-2011 |
20120142928 | PROCESS FOR THE PREPARATION OF CATHEPSIN S INHIBITORS - Inhibitors of Cathepsin S enzyme and their synthetic processes. | 06-07-2012 |
20120232275 | PROCESS FOR PREPARING 5-FLUORO-1H-PYRAZOLO [3,4-B] PYRIDIN-3-AMINE AND DERIVATIVES THEREOF - The present invention relates to a process for the synthesis of 5-fluoro-1H-pyrazolo[3,4-b]pyridin-3-amine in high yield and purity. The present invention also relates to processes for the synthesis of 5-fluoro-1H-pyrazolo[3,4-b]pyridin-3-amine derivatives. These processes are useful for preparing biologically active compounds, particularly certain GSK-3 inhibitors, or derivatives thereof. | 09-13-2012 |
20130197229 | METHOD OF MAKING AZAINDAZOLE DERIVATIVES - Disclosed are methods, reagents, and intermediates useful for making azaindazole derivatives, which may be used to modulate Glucokinase. The disclosed methods and materials are generally useful for making halo-esters and sulfonyl-substituted compounds. | 08-01-2013 |
20130303770 | RADIOLABELLED PHENYLIMIDAZOLE-BASED LIGANDS - The present invention relates to radiolabelled PDE10A ligands which are useful for imaging and quantifying the PDE10A enzyme using positron emission tomography (PET). | 11-14-2013 |
20140179924 | Process for the preparation of cathepsin S inhibitors - Inhibitors of Cathepsin S enzyme and their synthetic processes. | 06-26-2014 |
20140309425 | METHOD FOR SYNTHESIZING 1-(2-FLUOROBENZYL)-1H-PYRAZOLO[3,4-B]PYRIDINE-3-FORMAMIDINE HYDROCHLORIDE - The present invention relates to the field of chemical synthesis, and in particular to a method for synthesizing 1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-formamidine hydrochloride, which is an important intermediate of Riociguat that is an anti-thromboembolic-disease medicine. The method is characterized in that: 3-iodo-1H-pyrazolo[3,4-b]pyridine is used as a raw material; the raw material is reacted with fluorobenzyl bromide to form a compound (10); the compound (10) is reacted with zinc cyanide to form a compound (6); the compound (6) is reacted with sodium methoxide, ammonium chloride, acetic acid and methanol to form a compound (8); and the compound (8) is reacted with chlorine hydride gas to form 1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-formamidine hydrochloride. The method has the characteristics of cheap and readily available raw materials, high yield, mild reaction conditions and the like, and is a synthesis method having a large-scale preparation value. | 10-16-2014 |
20140350259 | PROCESS FOR THE PREPARATION OF 2-PHENYL-[1,2,4]TRIAZOLO[1,5-A]PYRIDINE DERIVATIVES - The invention relates to a novel process for the preparation of 2-phenyl-[1,2,4]triazolo[1,5-a]pyridine derivatives of formula I or of a salt thereof | 11-27-2014 |
20150148542 | METHOD FOR PREPARING SUBSTITUTED TRIAZOLOPYRIDINES - The present invention relates to methods of preparing substituted triazolopyridine compounds of general formula (I) as described and defined herein, as well as to intermediate compounds useful in the preparation of said compounds. | 05-28-2015 |
20160039813 | PROCESS FOR THE PREPARATION OF 4-(8-(2-CHLOROPHENOXY)-[1,2,4]TRIAZOLO[4,3-A]PYRIDIN-3-YL)BICYCLO[2.2.1]H- EPTAN-1-OL AND NOVEL INTERMEDIATES THEREFOR - A process is provided for preparing 4-(8-(2-chlorophenoxy)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)bicyclo[2.2.1]heptan-1-ol and novel intermediates used in the process. The compound is a 11-beta hydroxysteroid dehydrogenase type I inhibitor which exhibits activity in the treatment of various metabolic diseases. | 02-11-2016 |
546120000 | Having -C(=X)-, wherein X is chalcogen, bonded directly to the bicyclo ring system | 7 |
20120035370 | Azaindazole Compounds As CCR1 Receptor Antagonists - Disclosed are compounds of the formula (I), useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of CCR1 including autoimmune diseases, such as rheumatoid arthritis and multiple sclerosis. | 02-09-2012 |
20130211090 | METHOD FOR THE PRODUCTION OF 5-FLUORO-1H-PYRAZOLO[3,4-B]PYRIDINE-3-CARBONITRILE - The present invention relates to a process for preparing 5-fluoro-1H-pyrazolo[3,4-b]pyridine-3-carbonitrile of the formula (I) | 08-15-2013 |
20130245267 | NOVEL FORMS OF APIXABAN - The present application relate to amorphous form of Apixaban useful in making pharmaceutically acceptable dosage forms, and to processes for their preparation. | 09-19-2013 |
20140350260 | HETEROCYCLIC COMPOUND AND USE THEREOF - The present invention provides a heterocycle derivative having a superior amyloid β production inhibitory activity and/or a superior γ-secretase modulation activity, and use thereof. A compound represented by the formula (I): | 11-27-2014 |
20140378686 | Indanyl-Substituted 4,5,6,7-Tetrahydro-1H-Pyrazolo[4,3-C]Pyridines, Their Use as Medicament, and Pharmaceutical Preparations Comprising Them - The invention relates to substituted 4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridines of formula (I), their use as medicament, and pharmaceutical preparations comprising them. The compounds of formula (I) act on the TASK-1 potassium channel. The compounds are particularly suitable for the treatment or prevention of atrial arrhythmias, for example atrial fibrillation (AF) or atrial flutter. | 12-25-2014 |
20150353541 | Novel intermediate and polymorphs of 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetra hydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide and process thereof - The present invention provides a novel intermediate as well as novel polymorphs of 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide compound represented by the following structural formula-1 and processes for their preparation. | 12-10-2015 |
20150353543 | PROCESS FOR THE PREPARATION AND PURIFICATION OF APIXABAN - The present invention provides a process for the preparation and purification of apixaban. | 12-10-2015 |