Search

Process for the synthesis of Nangibotide

New approach to the synthesis of Propofol

New approach to the synthesis of Semaglutide side chain

A new base for FMOC deprotecion have bee described

New approach to the synthesis of Etecalcetide

The present invention relates to a process for the preparation of Treosulfan. The present invention also relates to a novel intermediate useful in the preparation of Treosulfan

The invention relates to a process for the preparation of ribociclib of formula V or its salts. The invention provides novel crystalline forms of ribociclib succinate and ribociclib trifluoroacetate. The present invention also relates to pharmaceutical compositions comprising a crystalline form of ribociclib succinate and at least a pharmaceutically acceptable carrier. It further relates to the use of such compositions in the treatment of cancer.

New process for the synthesis of glucagon

The present invention relates to a process for preparing Alectinib or a pharmaceutically acceptable salt thereof. The present invention also relates to novel polymorphic forms of Alectinib and Alectinib hydrochloride.

Process for the synthesis of glucagon

new process for the synthesis of degarelix

The present invention relates to a fragment based manufacturing process for abaloparatide, which is an analogue of parathyroid hormone related peptide (PTHrP), and its related intermediates resulting in a product with high yield and high purity.

The present invention relates to an improved process for the preparation of Venetoclax or its salt

new crystalline form of acalabrutinib

The present invention provides a process for the manufacture of GLP-1 analogues with high yield and purity by fragment condensation on the solid phase. In particular, it describes a convergent synthesis by condensation of a C-terminal pseudoproline fragment A with a fragment B bound to a solid support, followed by deprotection and cleavage from the support and final purification to yield the desired peptide. The invention further provides intermediates useful in the manufacturing process.

The present invention relates to a process for the preparation of compound of formula (I), wherein, R1 and R2 are each independently hydroxy, alkoxy, aryloxy, or aralkoxy; or R1 and R2 together form a moiety derived from an alpha-hydroxy carboxylic acid compound or a beta-hydroxy carboxylic acid compound, wherein the atom attached to boron in each case is an oxygen atom; or R1 and R2 together form the boronate esters of boronic acid.

The present invention relates to an improved process for the preparation of a compound of formula (I), wherein PG1 may be independently selected from tert-butyloxycarbonyl (Boc), phthaloyl, 9-fluorenylmethyloxycarbonyl (Fmoc), triphenylmethyl (Trityl), carboxybenzyl (Cbz), trifluoroacetyl, benzyl (Bn), benzylidene, methanesulfonyl (Mesyl), toluene sulfonyl (Tosyl) or acyl; its isolation as solid and use for the preparation of the compound of formula (IV), in particular the compound of formula (IV) i.e. [(1R)-3-methyl-1[[(2S)-1-oxo-3-phenyl-2- [(pyrazinylcarbonyl) amino]propyl]amino]butyl] boronic acid with more than 99.95% chiral purity, as measured by HPLC

The present invention relates to peptidomimetic synthesis. In particular, it relates to processes for the manufacture of antagonists of bradykinin B2 receptor. More in particular, the present invention relates to a process for the manufacture of icatibant by fragment condensation and to the preparation of such fragments.

The present invention relates to a process for the purification of compound of formula II, wherein X may be independently selected from trifluoroacetic acid, hydrochloric acid, hydrobromic acid, p-toluene sulfonic acid and phosphoric acid; its isolation as solid and use for the preparation of carfilzomib.

The present invention relates to an improved process for the preparation of xylene linked cyclam compounds. More particularly the invention provides a process for preparation of high purity plerixafor which does not involve the use of expensive chemicals, hazardous reagents or tedious purification techniques. Invention also provides novel intermediate useful for preparation of desired compound in high purity.

The present invention relates to the polymorphic forms of Belinostat. The invention also relates to the process for the preparation of the polymorphic forms of Belinostat. This invention further relates to pharmaceutical composition of said polymorphic forms of Belinostat and use thereof in the treatment of a patient in need thereof.

Liraglutide is a new generation lipopeptide drug used for the treatment of type II diabetes. In this work, we describe new approaches for its preparation fully by chemical methods. The key step of these strategies is the synthesis in solution of the Lys/γ-Glu building block, Fmoc-Lys-(Pal-γ-Glu-OtBu)-OH, in which Lys and Glu residues are linked through their side chains and γ-Glu is Nα-palmitoylated. This dipeptide derivative is then inserted into the peptide sequence on solid phase. As liraglutide is obtained with great purity and high yield, our approach can be particularly attractive for an industrial production. We also report here the results of a circular dichroism conformational analysis in a membrane mimetic environment that offers new insights into the mechanism of action of liraglutide. Copyright © 2016 European Peptide Society and John Wiley & Sons, Ltd

The present invention relates to crystalline forms of Afatinib and its dimaleate salt. The present invention also relates to processes for the preparation of crystalline forms of Afatinib and its dimaleate salt. The present invention further relates to pharmaceutical compositions of such crystalline forms of Afatinib dimaleate and use thereof in the treatment of a patient in need thereof

The present application provides an improved process for the preparation of sugammadex by reacting a salt of 3-mercapto propionic acid with 6-per-deoxy-6-per-halo-γ-cyclodextrin in a suitable organic solvent. This application also provides crystalline form of a salt of 3-mercapto propionic acid, preferably di sodium salt of 3-mercapto propionic acid and its use for the preparation of sugammadex, whereas formula (I) shows the sodium salt of sugammadex.

The present invention refers to an amorphous form of a thiocolchicine derivative, IDN 5404, to a process for producing it and to pharmaceutical compositions thereof. The amorphous form is characterised by the XRPD pattern, DSC profile and/or TG/DTA profile.

The present application provides an improved process for the preparation of sugammadex. More particularly, the application relates to an improved process for the preparation of 6-per-deoxy-6-per-halo-γ-cyclodextrin and optionally its isolation as a crystalline compound, wherein said halo is bromo or chloro. This application also relates to the use of said crystalline 6-per-deoxy-6-per-halo-γ-cyclodextrin for the preparation of sugammadex which improves overall yield and/or purity of sugammadex.

Carfilzomib The present invention relates to a process for the purification of Carfiizomib of Formula Ϊ that reduces the level of an acetaniide impurity of Formula II preferably below 0.10 wt%. Formula I Formula II.

The present application provides crystalline forms of 6-per-deoxy-6-per-chloro-γ-cyclodextrin, polymorphs thereof and methods to produce it. More particularly, the application relates to a process of dissolving 6-per-deoxy-6-per-chloro-γ-cyclodextrin and its isolation as a crystalline compound.

Ruthenium catalyzed 1,3-cycloaddition (click chemistry) of an azido moiety installed on dihydroxycumene scaffold with differently substituted aryl propiolates gave a new family of 1,4,5-trisubstituted triazole carboxylic acid derivatives that showed high affinity toward Hsp90 associated with cell proliferation inhibition, both in nanomolar range. The 1,5 arrangement of the resorcinol, the aryl moieties, and the presence of an alkyl (secondary) amide in position 4 of the triazole ring were essential to get high activity. Docking simulations suggested that the triazoles penetrate the Hsp90 ATP binding site. Some 1,4,5-trisubstituted triazole carboxamides induced dramatic depletion of the examined client proteins and a very strong increase in the expression levels of the chaperone Hsp70. In vitro metabolic stability and in vivo preliminary studies on selected compounds have shown promising results comparable to the potent Hsp90 inhibitor NVP-AUY922. One of them, (compound 18, SST0287CL1) was selected for further investigation as the most promising drug candidate.

Since its discovery in the 1940s in serum, the mammalian intestinal mucosa, and in the central nervous system, serotonin (5-HT) has been shown to be involved in virtually all cognitive and behavioral human functions, and alterations in its neurochemistry have been implicated in the etiology of a plethora of neuropsychiatric disorders. The cloning of 5-HT receptor subtypes has been of importance in enabling them to be classified as specific protein molecules encoded by specific genes. The 5-HT7 receptor is the most recently classified member of the serotonin receptor family. Since its identification, it has been the subject of intense research efforts driven by its presence in functionally relevant regions of the brain. The availability of some selective antagonists and agonists, in combination with genetically modified mice lacking the 5-HT7 receptor, has allowed for a better understanding of the pathophysiological role of this receptor. This paper reviews data on localization and pharmacological properties of the 5-HT7 receptor, and summarizes the results of structure-activity relationship studies aimed at the discovery of selective 5-HT7 receptor ligands. Additionally, an overview of the potential therapeutic applications of 5-HT7 receptor agonists and antagonists in central nervous system disorders is presented.

Natural colchicinoids and their semisynthetic derivatives are important active ingredients for pharmaceutical applications. Thiocolchicoside (3-demethoxy-3-glucosyloxythiocolchicine) is used in several countries as standard therapy for the treatment of diseases of the muscle-skeletal system, due to its potent antiinflammatory and myorelaxant properties. Manufacturing of thiocolchicoside requires a key step, the regioselective demethylation and glucosylation of chemically derivative thiocolchicine. High selectivity and efficiency of this transformation cannot be achieved in a satisfactory way with a chemical approach. In particular, the chemical demethylation, a part from requiring toxic and aggressive reagents, generates a complex mixture of products with no industrial usefulness. We report herein an efficient, direct and green biotransformation of thiocolchicine into thiocolchicoside, performed by a specific strain of Bacillus megaterium. The same process, with minor modifications, can be used to convert the by-product 3-O-demethyl-thiocolchicine into thiocolchicoside. In addition, we describe the B. megaterium strain selection process and the best conditions for this effective double biotransformation. The final product has a pharmaceutical quality, and the process has been industrialised.

The present invention refers to an amorphous form of a thiocolchicine derivative, IDN 5404, to a process for producing it and to pharmaceutical compositions thereof. The amorphous form is characterised by the XRPD pattern, DSC profile and/or TG/DTA profile.

The synthesis and preliminary in vitro evaluation of five metabolites of the A2A antagonist ST1535 (1) are reported. The metabolites, originating in vivo from enzymatic oxidation of the 2-butyl group of the parent compound, were synthesized from 6-chloro-2-iodo-9-methyl-9H-purine (2) by selective C-C bond formation via halogen/magnesium exchange reaction and/or palladium-catalyzed reactions. The metabolites behaved in vitro as antagonist ligands of cloned human A2A receptor with affinities (Ki 7.5-53 nM) comparable to that of compound 1 (Ki 10.7 nM), thus showing that the long duration of action of 1 could be in part due to its metabolites. General behavior after oral administration in mice was also analyzed.

The present invention relates to a new crystalline form of Cabazitaxel, to a process for the preparation and to pharmaceutical compositions thereof

BREVETTO CONCESSO new HDAC inhibitors bearing a thiol as zinc chlating agent are descebed

BREVETTO CONCESSO The patent describes a novel process for the synthesis of 7-chloro-4-(piperazin-1-yl)-quinoline and a new crystalline form

The present invention relates to aryl triazole derivatives of Formula I having antitumoural activity through, as one possible biological target, the molecular chaperone heat shock protein 90 (Hsp90) inhibition. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of Hsp90 is responsive, and the pharmaceutical composition containing such compounds.

The Future of Pharma INdustry

BREVETTO CONCESSO The present invention relates to new triazolyl purine derivatives of formula (I), processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders or cerebral ischaemia for which inhibition of adenosine A2A receptor will result at improving the health state of a patient

The present invention relates to new carbamate derivatives of formula I, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of neurological disorders, such as neuropathic pain and anxiety.

The present invention relates to novel amide compounds of formula I, and their use as anti-tumoral and pro-apoptotic agents. The invention includes the use of such compounds in medicine, in relation to cancer disease as well as other diseases where an inhibition of HDAC6 is responsive, and the pharmaceutical composition containing such compounds.

BREVETTO CONCESSO A stereoselective process for preparing 7-[(E)-t-butyloxyiminomethyl]-camptothecin (also known as gimatecan) is herein disclosed. With the addition of further dissolution and precipitation steps carried out in appropriate different solvent mixtures, four new crystalline forms of gimatecan are also obtainable by using the same stereoselective process.