| Class / Patent application number | Description | Number of patent applications / Date published |
|---|
| 548469000 |
The bicyclo ring system consists of the five-membered hetero ring and a benzene ring (e.g., indole, etc.)
| 128 |
| 548465000 |
Additional hetero ring, attached directly or indirectly to the bicyclo ring system by nonionic bonding
| 34 |
| 548454000 |
Additional polycyclo heterocyclic ring system attached directly or indirectly to the bicyclo ring system by nonionic bonding
| 21 |
| 548453000 |
Plural ring hetero atoms in the bicyclo ring system, or ring nitrogen is shared by the two cyclos of the bicyclo ring system
| 14 |
| 548515000 |
The ring nitrogen is bonded directly to two ring carbons of the same cyclo which carbons are members of one cyclo only (e.g., cyclopenta(c)pyrroles, etc.)
| 10 |
| 548512000 |
Chalcogen bonded directly to ring carbon of the five-membered hetero ring (e.g., adrenochrome, etc.) | 4 |
| 20090240063 | Process For The Preparation Of 6,6-Dimethyl-3-Azabicyclo-[3.1.0]-Hexane Compounds ... - The present invention provides for a process for preparing racemic methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate, its corresponding salt: (2S, 3R, 4S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-D-tartaric acid (“D-DTTA”) salt or a (2R, 3S, 4R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate di-p-toluoyl-L-tartaric acid salt (“L-DTTA”) in a high enantiomeric excess. This invention also provides for a process for preparing a (2S, 3R, 4S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate dibenzoyl-D-tartaric acid (“D-DBTA”) salt or a (2R, 3S, 4R)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylate L-tartaric acid (“L-DBTA”) salt in a high enantiomeric excess. Further, this invention provides a process for preparing intermediates II, IIB, III, IV, IV salt, V, VI, and VII. | 09-24-2009 |
| 20140142322 | Boronic Acid Catalysts and Methods of Use Thereof for Activation and Transformation of Carboxylic Acids - The present application provides methods and catalysts for activation of carboxylic acids for organic reactions. In particular, methods are disclosed for direct nucleophilic addition reactions, such as, amidation reactions with amines, cycloadditions, and conjugate additions, using boronic acid catalysts of formula I, II or III: Also included are novel boronic acid catalysts of formula IV, V and III: | 05-22-2014 |
| 20100145069 | PROCESS FOR THE PREPARATION OF 6,6-DIMETHYL-3-AZABICYCLO-[3.1.0]- HEXANE COMPOUNDS UTILIZING BISULFITE INTERMEDIATE - The present invention provides for a process for preparing 6,6-Dimethyl-3-aza-bicyclo[3.1.0]hexane-2-sulfonate, an intermediateuseful in the efficient preparation of (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylic acid and esters and salts thereof, processes for preparing (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylic acid and esters and salts thereof from the sulfonate intermediate and processes for preparing 6,6-Dimethyl-3-aza-bicyclo[3.1.0]hexane-2-sulfonate. | 06-10-2010 |
| 20140094616 | PROCESS FOR PRODUCING ESTER COMPOUND - Compound (1) or a salt that is useful as an intermediate for the production of a medicine, an agrochemical or the like can be produced by a process including the following steps: (A) reacting an aldehyde (2) with nitromethane to produce a nitroaldehyde; (B) reacting the nitroaldehyde with an alcohol to produce a nitroacetal; (C) reducing the nitroacetal to produce an aminoacetal; (D) protecting an amino group in the aminoacetal to produce a protected aminoacetal; (E) treating the protected aminoacetal with an acid and subsequently with a base and then reacting the resultant product with a cyanating agent to produce a nitrile; (F) hydrolyzing the nitrile to produce a protected amino acid; and (G) substituting a group R | 04-03-2014 |
| Entries |
| Document | Title | Date |
|---|
| 20080234493 | Process for the Preparation of 2-[N-[{S)-1-Ethoxycarbonyl-3-Phenylpropyl]-(S)-Alanyl]-(1S,3S,5S)-2-Azabicyclo[3.3.0]Oct- an-3-Carboxylic Acid - A process for preparation of 2-[N-[(S)-1-ethoxycarbonyl-3-phenylpropyl]-(S)-alanyl]-(1S,3S,5S)-2- azabicyclo [3.3.0] octane-3-carboxylic acid, ie. Ramipril, involves condensation of an activated derivative of 2-[N-](S)-1-ethoxycarbonyl-3-phenylpropyl]-(S)-alanine with racemic (1R*,3R*,5R*)-2-azabicyclo[3.3.0]octane-3-carboxylic acid, and then the desired diastereoisomer (1a) is separated from the obtained diastereoisomeric mixture of 2-[N-[(S)-1-ethoxycarbonyl-3-phenylpropyl](S)-alanyl]-(1S,3S,5S)-2-azabicyclo[3.3.0]octane-3-carboxylic acid (1a) and 2-[N-[(S)-1-ethoxycarbonyl-3-phenylpropyl -alanyl]-(1R,3R,5R)-2-azabicyclo[3.3.0]octane-3-carboxylic acid (1b) by treating it with a solvent that selectively dissolves the undesired diastereoisomer (1b) while the diastereoisomer (1a) remains undissolved. | 09-25-2008 |
| 20090099370 | Crystalline Form of Perindopril Erbumine - The present invention relates to new crystalline form of the ACE inhibitor perindopril and processes for the preparation thereof. | 04-16-2009 |
| 20090281331 | METHOD OF PRODUCING POLYCYCLIC PROLINE DERIVATIVE OR ACID ADDITION SALT THEREOF - A process for producing proline derivatives of formula (1) below or acid adduct salts thereof, including: the step of reacting N-protected pyrrolidinones of formula (2) below with reducing agents to thereby obtain N-protected pyrrolidinols of formula (3) below (step A); the step of reacting the N-protected pyrrolidinols obtained in the step A with cyanating agents to thereby obtain N-protected cyanopyrrolidines of formula (4) below (step B); the step of reacting the N-protected cyanopyrrolidines obtained in the step B with alcohols and bases to thereby obtain imidates of formula (5) below and treating the imidates with acids to thereby obtain N-protected prolines of formula (6) below (step C); and the step of treating the N-protected prolines obtained in the step C with acids (step D). In formulas (1)-(6) below, any two out of R | 11-12-2009 |
| 20090306404 | Process for the Preparation of 2-azabicyclo[3.3.0]octane-3-carboxylic Acid Derivatives - The present invention is aimed at a process for the preparation of compounds of the general formula (I). | 12-10-2009 |
| 20090326244 | BISULFITE PURIFICATION OF AN ALPHA-KETO AMIDE - A process for purifying the alpha-keto amide is (1R,5S)—N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]-amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide via a bisulfite adduct is disclosed. | 12-31-2009 |
| 20100010235 | Method of using rhodium quinonoid catalysts - In accordance with aspects of the invention methods of using rhodium hydroquinone catalysts for the conjugate addition of boronic acids are disclosed. | 01-14-2010 |
| 20100016614 | PROCESS FOR THE PREPARATION OF PERINDOPRIL ERBUMINE - The present invention relates to a new process for the preparation of pure perindopril erbumine. The present invention also relates to a new process for the preparation of crystalline form D of perindopril erbumine. | 01-21-2010 |
| 20100063300 | BIOCATALYTIC PROCESSES FOR THE PREPARATION OF SUBSTANTIALLY STEREOMERICALLY PURE FUSED BICYCLIC PROLINE COMPOUNDS - The present disclosure provides substantially enantiomerically pure heterobicyclic compounds of the following structural formulas, | 03-11-2010 |
| 20100204486 | Process for the Synthesis of (+)and (-)-1 Aryl-3-Azabicyclo(3.1.0) Hexanes - The present invention is concerned with novel processes for the preparation of (+)-1-aryl-3-azabicyclo[3,10]hexanes or a pharmaceutically acceptable salt thereof, and (−)-1-aryl-3-azabicyclo[3,10]hexanes or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., pain, depression, anxiety disorders, eating disorders and urinary incontinence. | 08-12-2010 |
| 20100274025 | METHODS AND COMPOUNDS FOR PRODUCING DIPEPTIDYL PEPTIDASE IV INHIBITORS AND INTERMEDIATES THEREOF - Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided. | 10-28-2010 |
| 20100298574 | Process For The Synthesis Of (+) And (-)-1-(3,4-Dichlorophenyl)-3-Azabicyclo[3.1.0]Hexane - The present invention is concerned with novel processes for the preparation of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and (−)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. These compounds have pharmaceutical utility and are known to be useful for treating e.g., depression, anxiety disorders, eating disorders and urinary incontinence. | 11-25-2010 |
| 20100324304 | IMPROVED RAMIPRIL SYNTHESIS - The present invention relates to the preparation of ramipril (formula [1]) from unprotected (2S,3S,6S)-octahydrocyclopenta[b]pyrrole-2-carboxylic acid and to a method for preparing unprotected (2S,3S,6S)-octahydrocyclopenta[b]pyrrole-2-carboxylic acid. | 12-23-2010 |
| 20110092716 | DEHYDROHALOGENATION PROCESS FOR THE PREPARATION OF INTERMEDIATES USEFUL IN PROVIDING 6,6-DIMETHYL-3-AZABICYCLO-[3.1.0]- HEXANE COMPOUNDS - The present invention provides for a process for preparing the pyrrole compounds of Formula Va and Vb. | 04-21-2011 |
| 20110144352 | PROCESSES FOR THE PREPARATION OF 4-OXO-OCTAHYDRO-INDOLE-1-CARBOCYCLIC ACID METHYL ESTER AND DERIVATIVES THEREOF - The present invention relates to a process for the production of carbamic acid (2-chloroethyl)(3-oxocyclohexyl)-alkyl ester enantiomers and of 1-carbalkoxy-4-ketoperhydroindole enantiomers. | 06-16-2011 |
| 20110263871 | METHOD FOR THE SYNTHESIS OF A RAMIPRIL INTERMEDIATE - The present invention relates to a process for the preparation of octahydrocyclopenta[b]pyrrole-2-carboxylic acid and esters thereof of general formula (1) in the presence of a cobalt and/or nickel comprising catalyst and to the use of compounds of general formula (1) in the synthesis of ramipril. | 10-27-2011 |
| 20110301357 | NOVEL POLYMORPHIC FORMS OF PERINDOPRIL (L)-ARGININE AND PROCESS FOR THE PREPARATION THEREOF - The present invention relates to novel and stable polymorphic forms of Perindopril (L)-Arginine designated as Form γ and amorphous form and processes for their preparation. The present invention also provides the novel polymorph Form γ with greater stability to heat and humidity and can be prepared on large scale by an efficient, economic and reproducible process. | 12-08-2011 |
| 20120178942 | ENANTIO- AND STEREO-SPECIFIC SYNTHESES OF BETA-AMINO-ALPHA- HYDROXY AMIDES - Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed. | 07-12-2012 |
| 20120259129 | Process for Preparing Azabicyclic Compounds - The present invention relates to a process for preparing azabicyclic compounds that are useful intermediates for synthesizing pharmaceutical compounds or salts thereof. | 10-11-2012 |
| 20130012723 | METHODS AND COMPOUNDS FOR PRODUCING DIPEPTIDYL PEPTIDASE IV INHIBITORS AND INTERMEDIATES THEREOF - Methods and compounds for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV are provided. | 01-10-2013 |
| 20130023671 | PROCESS FOR PREPARING SAXAGLIPTIN AND ITS NOVEL INTERMEDIATES USEFUL IN THE SYNTHESIS THEREOF - Methods of making saxagliptin, pharmaceutically acceptable salts and hydrates thereof and intermediates thereof. | 01-24-2013 |
| 20130178635 | PROCESS FOR THE PREPARATION OF THE L-ARGININE SALT OF PERINDOPRIL - Process for the preparation of the compound of formula (I): | 07-11-2013 |
| 20130204012 | Process For Preparing Dipeptidyl Peptidase IV Inhibitors And Intermediates Therefor - A process for production of cyclopropyl-fused pyrrolidine-based inhibitors of dipeptidyl peptidase IV is provided which employs a BOC-protected amine of the structure | 08-08-2013 |
| 20130317235 | PROCESS FOR THE PREPARATION OF (1S, 3S, 5S)-2-[2(S)-2-AMINO-2-(3-HYDROXY-1-ADAMANTAN-1-YL ACETYL]-2-AZABICYCLO [3.1.0] HEXANE-3-CARBONITRILE - The present invention relates to an improved process for the preparation of (1S,3S,5S)-242(S)-2-amino-2-(3-hydroxy-1-adamantan-1-yl)acetyl]-2-azabicyclo[3.1.0]hexane-3-carbonitrile and its intermediates. | 11-28-2013 |
| 20140135504 | NOVEL POLYMORPHIC FORMS OF PERINDOPRIL (L)-ARGININE AND PROCESS FOR THE PREPARATION THEREOF - The present invention relates to novel and stable polymorphic forms of Perindopril (L)-Arginine designated as Form γ and amorphous form and processes for their preparation. The present invention also provides the novel polymorph Form γ with greater stability to heat and humidity and can be prepared on large scale by an efficient, economic and reproducible process. | 05-15-2014 |
| 20140336393 | PROCESS FOR PREPARING MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR - The present invention relates to processes for preparing solid state forms of N-(4-(7-azabicyclo[2.2.1]heptan-7-yl)-2-(trifluoromethyl)phenyl)-4-oxo-5-(trifluoromethyl)-1,4-dihydroquinoline-3-carboxamide, including Compound 1 Form A, Compound 1 Form A-HCl, Compound 1 Form B, and Compound 1 Form B-HCl, any combination of these forms, pharmaceutical compositions thereof, and methods of treatment therewith. | 11-13-2014 |
| 20150112084 | PROCESS FOR PREPARATION OF (IS, 3S, 5S)-2-[(2S)-2-AMIN0-2-(3-HYDROXY-l-ADAMANTYL) ACETYL]-2-AZABICYCLO [3.1.0] HEXANE-3-CARBONITRILE - Provided are novel processes for the preparation of Saxagliptin and novel intermediates employed in the process for preparing Saxagliptin. | 04-23-2015 |
| 20150329489 | SAXAGLIPTIN SALTS - The present invention provides saxagliptin bisulphate, saxagliptin acetate, saxagliptin oxalate, saxagliptin bicarbonate, and saxagliptin carbonate, their polymorphic forms, processes for their preparation, and pharmaceutical compositions thereof. | 11-19-2015 |
| 20150336890 | NOVEL POLYMORPHIC FORMS OF PERINDOPRIL (L)-ARGININE AND PROCESS FOR THE PREPARATION THEREOF - The present invention relates to novel and stable polymorphic forms of Perindopril (L)-Arginine designated as Form γ and amorphous form and processes for their preparation. The present invention also provides the novel polymorph Form γ with greater stability to heat and humidity and can be prepared on large scale by an efficient, economic and reproducible process. | 11-26-2015 |
| 20160107992 | INTERMEDIATES USEFUL FOR THE PREPARATION OF SAXAGLIPTIN - Intermediates useful for the synthesis of saxagliptin and their preparationare described. | 04-21-2016 |
| 20160194282 | A Process For Preparation Of Saxagliptin And Its Hydrochloride Salt | 07-07-2016 |
