Class / Patent application number | Description | Number of patent applications / Date published |
548465000 | Additional hetero ring, attached directly or indirectly to the bicyclo ring system by nonionic bonding | 34 |
20080269502 | Process for the preparation of macrocyclic compounds - The present invention relates to a new process for the preparation of diene compounds of the | 10-30-2008 |
20110118477 | SUNITINIB AND SALTS THEREOF AND THEIR POLYMORPHS - Process for the preparation of sunitinib malate form I via sunitinib acetate and polymorphs of said intermediate. | 05-19-2011 |
20120271056 | PROCESS FOR THE PREPARATION OF CRYSTALLINE FORM I OF L-MALIC ACID SALT OF SUNITINIB - The present invention relates to a process for the preparation of crystalline Form I of the L-malic acid salt of sunitinib. | 10-25-2012 |
20130030192 | Method of Synthesizing Acetonide-Protected Catechol-Containing Compounds and Intermediates Produced Therein - The inventors disclose here a novel, facile approach to the synthesis of acetonide-protected catechol-containing compounds having at least one amine group. In specific embodiments, the invention provides novel methods of synthesizing 3,4-dihydroxyphenylalanine (H-DOPA(acetonide)-OH (6)), Fmoc-protected H-DOPA(acetonide)-OH (Fmoc-DOPA(acetonide)-OH (7)), Fmoc-protected dopamine (Fmoc-dopamine(acetonide) (10)), TFA-protected dopamine (TFA-dopamine(acetonide) (13)) and acetonide-protected 4-(2-aminoethyl)benzene-1,2-diol (acetonide-protected dopamine (14)). | 01-31-2013 |
20140187794 | Process for Preparing Chiral Compounds - The present invention is directed to a 2-deoxyribose-5-phosphate aldolase (DERA) chemoenzymatic process for making chiral compounds. | 07-03-2014 |
548466000 | The additional hetero ring is bonded directly to a ring carbon of the bicyclo ring system | 4 |
20080234494 | Indolylmaleimide Derivatives - A compound of formula I | 09-25-2008 |
20110021785 | NOVEL INDOLE DERIVATIVES AS SELECTIVE ANDROGEN RECEPTOR MODULATORS (SARMS) - The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor. | 01-27-2011 |
20130338374 | GPR 17 AGONISTS AND SCREENING ASSAY - The present invention is related to a method of determining a test compound's ability to modify the biological activity of a GPR17. Said method comprises, among others, the step of contacting the test compound with a GPR17, or a functional GPR17 fragment in the presence of a suitable amount of a GPR17 agonist of formula I. | 12-19-2013 |
20150133678 | ORGANIC COMPOUNDS CONTAINING SQUARIC ACID OR CROCONIC ACID MOIETIES FOR APPLICATION IN ELECTRONIC DEVICES - A compound containing a squaric acid or a croconic acid group as an anchoring group. The compound containing a squaric acid or a croconic acid group has formula 1: | 05-14-2015 |
548467000 | Substituent on ring carbon of the bicyclo ring system contains the additional hetero ring | 25 |
20080234495 | Process for the Preparation of Almotriptan - The present invention encompasses a method for the preparation of Almotriptan and its pharmaceutically acceptable salts comprises, i) Methylation of 3-[5-(1-Pyrrolidinyl sulfonyl methyl) 1H-indol-yl]ethane amine ii) Treating crude Almotriptan with a hydroxy benzoic acid yields hydroxy benzoic acid addition salt of Almotriptan iii) Converting Almotriptan hydroxy benzoic acid addition salt to Almotriptan and iv) Salification of Almotriptan to its pharmaceutically acceptable salts | 09-25-2008 |
20100004463 | PROCESS FOR SYNTHESIZING CARBAPENEM USING RANEY NICKEL - Convenient method for obtaining carbapenem by hydrogenation with Raney Nickel, as an alternative to the known catalytic hydrogenation conducted under hydrogen overpressure in the presence of Palladium, starting from corresponding protected intermediates such as p-nitrobenzylesters and with optional suitable protections of any primary and secondary amino functions structurally present. | 01-07-2010 |
20100022783 | CYCLOHEXANECARBOXYLIC ACID COMPOUND - The present invention provides a VLA-4 inhibitor having high water-solubility and excellent long-term stability; i.e., sodium trans-4-[1-[2,5-dichloro-4-[(1-methyl-1H-3-indolylcarbonyl)amino]phenylacetyl]-(4S)-methoxy-(2S)-pyrrolidinylmethoxy]cyclohexanecarboxylate pentahydrate. | 01-28-2010 |
20100076202 | METHOD FOR PRODUCING PYRROLIDINE DERIVATIVE - The present invention provides an advantageous method for producing an intermediate which is useful for production of a compound which exhibits excellent VLA-4 inhibitory effect and safety. | 03-25-2010 |
20100087659 | NORBORNENE COMPOUNDS WITH CROSS-LINKABLE GROUPS AND THEIR DERIVATIVES - The present invention provided a norbornene compound with cross-linkable groups and their derivative polymers, wherein said cross-linkable groups were olefin or epoxy groups. Norbornene polymers with cross-linkable side chain and their block copolymers as well as modified derivatives were prepared via living ring-open metathesis polymerization method. The resulting polymers with excellent solubility and optic properties had narrow molecular weight distribution, well-controlled molecular weight, small refraction index and high transparency. They were also suitable for preparing hybrid materials with high thermal stability and chemical resistance. | 04-08-2010 |
20150038726 | PROCESS FOR THE PREPARATION OF CARBAPENEM ANTIBIOTIC - The present invention provides an improved process for the preparation Ertapenem monosodium of formula (I) having purity greater than 98.5% and having pharmaceutically acceptable level of palladium and residual solvent. (I) | 02-05-2015 |
548468000 | The additional hetero ring and the bicyclo ring system are attached directly to the same acyclic carbon or acyclic carbon chain | 19 |
20080319205 | Process for preparing 5-bromo-3-[(R)-1-methyl-pyrrolidin-2-ylmethyl]-1H-indole - The invention encompasses a process for preparing 5-bromo-3-[(R)-1-methyl-pyrrolidin-2-ylmethyl]-1H-indole comprising reacting (R)-2-(5-bromo-1H-indole-3-carbonyl)-pyrrolidine-1-carboxylic acid benzyl ester with a reducing agent selected from the group consisting of sodium dihydro-bis(2-methoxyethoxy)aluminate, lithium tris[(3-ethyl-3-pentyl)oxy]aluminohydride, lithium tri-tert-butoxyaluminum hydride and diisobutylaluminium hydride. 5-bromo-3-[(R)-1-methyl-pyrrolidin-2-ylmethyl]-1H-indole is a key intermediate for preparing eletriptan and its salts thereof. | 12-25-2008 |
20090247767 | PROCESSES FOR PREPARING SUNITINIB AND SALTS THEREOF - Methods for preparing sunitinib or salts thereof are described using novel intermediates and chemical pathways. One such intermediate is: | 10-01-2009 |
20090299077 | Salts of (R)-5-(2phenylsulphonylethenyl)-3-(N-methylpyrrolidin-2-ylmethyl)- -1H-indole, 5-bromo-3-[(R)-1-methyl-pyrrolidin-2-ylmethyl]-1H-indole and of eletriptan - The present invention relates to salts of (R)-5-(2-phenylsulphonylethenyl)-3-(N-methylpyrrolidin-2-ylmethyl)-1H-indole of the formula: | 12-03-2009 |
20100160646 | PROCESSES FOR PREPARING SUNITINIB AND SALTS THEREOF - Methods for preparing sunitinib or salts thereof are described using novel intermediates and chemical pathways. One such intermediate is: | 06-24-2010 |
20110034703 | CRYSTAL FORMS OF N-[2-(DIETHYLAMINO)ETHYL]-5-[(5-FLUORO-1,2-DIHYDRO-2-OXO-3H-INDOL-3-YLIDE- NE)METHYL]-2,4-DIMETHYL-1H-PYRROLE-3-CARBOXAMIDE AND METHODS FOR THEIR PREPARATION - The present invention relates to novel crystal forms of Sunitinib and methods for their preparation. | 02-10-2011 |
20110092717 | PROCESS FOR THE PREPARATION OF HIGH PURITY SUNITINIB AND ITS PHARMACEUTICALLY ACCEPTABLE SALT - The present invention relates to an improved process for the preparation of N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide—Sunitinib base of formula (I) and its pharmaceutically acceptable malate salt of formula (I(a)). | 04-21-2011 |
20110166364 | SYNTHESIS OF 3--5-[2-(PHENYLSULFONYL)ETHYL]-1H-INDOLE - The present invention refers to the synthesis of 3-{[(2R)-1-methylpyrrolidin-2-yl]methyl}-5-[2-(phenylsulfonyl)ethyl]-1H-indole, a drug known by the name Eletriptan, or of its salts. In particular, the present invention regards a process for the synthesis of Eletriptan or of its salt, comprising the following steps: a) Salifying the intermediate of Formula (6), using a dicarboxylic acid to obtain a derived salt; b) Optionally, purifying said raw salt obtained according to step a) by solvent crystallization to obtain a purified salt of the intermediate of Formula (6); c) Converting said salt of the intermediate of formula (6) according to step a) or said purified salt according to step b) into an intermediate of formula (10); d) Converting the intermediate of Formula (10) into Eletriptan or its salt. | 07-07-2011 |
20110207943 | NOVEL PROCESS FOR THE PREPARATION OF ELETRIPTAN - The present invention relates to a novel process for the preparation of (R)-3-((1-methylpyrrolidin-2-yl)methyl)-5-(2-(phenylsulfonyl)ethyl)-1H-indole and its intermediates thereof. | 08-25-2011 |
20120071669 | PROCESS FOR PREPARATION OF ELETRIPTAN AND SALT THEREOF - The present invention relates to an improved process for the preparation of 3-(N-methyl-2(R)-pyrrolidinyl methyl)-5-[2-(phenyl sulfonyl)ethyl]-1H-indole or pharmaceutically acceptable salts thereof, particularly 3-(N-methyl-2(R)-pyrrolidinyl methyl)-5-[2-(phenyl sulfonyl)ethyl]-1H-indole hydrobromide (Eletriptan hydrobromide). The present invention further relates to novel polymorphs of 3-(N-methyl-2(R)-pyrrolidinyl methyl)-5-[2-(phenyl sulfonyl)ethenyl]-1H-indole hydrobromide and process for preparation thereof. | 03-22-2012 |
20120220783 | SALTS OF SUNITINIB - The present invention relates to salts of sunitinib and their preparation. | 08-30-2012 |
20130023672 | PROCESS FOR PREPARING ELETRIPTAN HYDROBROMIDE HAVING a-FORM - A process for preparation of eletriptan hydrobromide having a-form of formula (I) is described that includes reducing 3-((R)-1-methylpyrrolidin-2-yl)methyl)-5-((E)-2-(phenylsulfonyl)vinyl)-1H-indole of formula (II) in presence of a metal catalyst to the product of formula (III) and then converting to hydrobromide salt having a-form of formula (I). | 01-24-2013 |
20130123511 | PROCESS FOR THE DIRECT PREPARATION OF MALIC ACID SALT OF SUNITINIB - The present invention relates to a process for the direct preparation of malic acid salt of sunitinib. | 05-16-2013 |
20130190512 | PROCESSES FOR THE PREPARATION OF 3-(PYRROL-2-YL)METHYLENE)-2-PYRROLONES USING 2-SILYLOXY-PYRROLES - The present invention provides for synthetic processes for the making of substituted 3-((pyrrol-2-yl)methylene)-2-pyrrolones, including sunitinib. The present invention also provides for a process of crystallizing substantially pure sunitinib L-malate. | 07-25-2013 |
20130197242 | PROCESS FOR THE PREPARATION OF CRYSTALLINE FORM II OF L-MALIC ACID SALT OF SUNITINIB - The present invention relates to stable crystalline Form II of L-malic acid salt of sunitinib and its preparation. | 08-01-2013 |
20130296575 | SUNITINIB AND SALTS THEREOF AND THEIR POLYMORPHS - Process for the preparation of sunitinib malate form I via sunitinib acetate and polymorphs of said intermediate. | 11-07-2013 |
20150025252 | PROCESS FOR THE PERPARATION OF SUNITINIB AND ITS ACID ADDITION SALTS THEREOF - The present invention relates to an improved process for the preparation of Sunitinb. The process involves the activation of 5-((Z)-(5-fluoro-2-oxoindolin-3-ylidene) methyl)-2,4-dimethyl-1H-pyrrole-3carboxylic acid to corresponding suitable carboxylic acid activating group. The present invention also relates to novel acid addition salts of Sunitinb and preparation thereof. | 01-22-2015 |
20150045562 | Chemical Process for Preparing Spiroindolones and Intermediates Thereof - The present invention relates to processes and intermediates useful for the manufacture of spiroindolone compounds such as (1′R,3′S)-5,7′-dichloro-6′-fluoro-3′-methyl-2′,3′,4′,9′-tetrahydrospiro[indoline-3,1′-pyrido[3,4-b]indol]-2-one and salts and hydrates and solvates thereof. | 02-12-2015 |
20150112085 | PURE CRYSTALLINE FORM II OF L-MALIC ACID SALT OF SUNITINIB AND PROCESSES FOR ITS PREPARATION - The present invention relates to pure crystalline Form II of an L-malic acid salt of sunitinib and a process for its preparation. The invention further provides crystalline Form II of an L-malic acid salt of sunitinib having a purity of at least 97.0%. The invention also provides crystalline Form II of an L-malic acid salt of sunitinib substantially free of an anti-oxidant. The invention also provides crystalline Form II of L-malic acid salt of sunitinib which remains chemically pure on storage at 25° C.±2° C. and 40° C.±2° C. at a relative humidity of 60%±5% and 75%±5%, respectively, for at least 1 month. | 04-23-2015 |
20160185760 | PROCESS FOR THE PREPARATION OF MALIC ACID SALT OF SUNITINIB - The present invention relates to a process of preparation of malic acid salt of sunitinib.(I). | 06-30-2016 |