The invention relates to solid state forms of Cabazitaxel, and processes for preparation, via novel synthetic intermediates, thereof, and formulations comprising one or more of the solid state forms of Cabazitaxel. The present invention further provides pharmaceutical compositions comprising one or more of the solid state forms of Cabazitaxel, and a method of treating hormone-refractory prostate cancer.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
2.
SOLID STATE FORMS OF CABAZITAXEL AND PROCESSES FOR PREPARATION THEREOF
The invention relates to solid state forms of Cabazitaxel and processes for preparing the solid state forms. The invention further relates to pharmaceutical compositions and formulations comprising one or more of the solid state forms.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
Processes for preparing and purifying Pralatrexate are described in the present application, as well as intermediates in these processes, and salts and solid state forms of the Pralatrexate intermediates.
C07D 475/08 - Heterocyclic compounds containing pteridine ring systems with a nitrogen atom directly attached in position 4 with a nitrogen atom directly attached in position 2
4.
SOLID STATE FORMS OF CABAZITAXEL AND PROCESSES FOR PREPARATION THEREOF
The invention relates to solid state forms of Cabazitaxel, and processes for preparation, via novel synthetic intermediates, thereof, and formulations comprising one or more of the solid state forms of Cabazitaxel. The present invention further provides pharmaceutical compositions comprising one or more of the solid state forms of Cabazitaxel, and a method of treating hormone-refractory prostate cancer.
C07D 305/14 - Heterocyclic compounds containing four-membered rings having one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
A61K 31/337 - Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having four-membered rings, e.g. taxol
Crystalline forms of Dabigatran Etexilate and Dabigatran Etexilate mesylate are described in the present application and processes for preparing the crystalline forms. The present invention also includes pharmaceutical compositions of such crystalline forms of Dabigatran Etexilate and Dabigatran Etexilate mesylate, methods of their preparation and the use of such crystalline forms in the treatment of a patient in need thereof.
C07D 401/12 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
A61K 31/4439 - Non-condensed pyridinesHydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
Crystalline forms of Ixabepilone are described in the present application and processes for preparing the crystalline forms. The present invention also includes pharmaceutical compositions of such crystalline forms of Ixabepilone.
Compounds useful in the preparation of telavancin, for example, were prepared. These compounds include decylaminoethanal dialkyl acetals and N-protected decylaminoethanal dialkyl acetals, imidazolidine derivatives, and N-protected- decylaminoethanal.
C07C 217/28 - Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having one amino group and at least two singly-bound oxygen atoms, with at least one being part of an etherified hydroxy group, bound to the carbon skeleton, e.g. ethers of polyhydroxy amines
C07C 271/16 - Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
C07D 233/02 - Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
C07K 9/00 - Peptides having up to 20 amino acids, containing saccharide radicals and having a fully defined sequenceDerivatives thereof
8.
POLYMORPHS OF BENDAMUSTINE HCL AND PROCESSES FOR PREPARATION THEREOF
Novel polymorphs of Bendamustine HC1 have been prepared and characterized. These polymorphs and pharmaceutical compositions containing them are useful, for example, in treating patients with various cancers.
A61K 31/4184 - 1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
C07D 235/16 - Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
The present invention provides crystalline forms of Fluticasone furoate, characterized by the data disclosed in the specification; pharmaceutical compositions comprising any one or combination of the crystalline forms of Fluticasone furoate and at least one pharmaceutically acceptable excipient; and the use of the crystalline forms of Fluticasone furoate in the preparation of pharmaceutical formulations.
C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61P 5/44 - GlucocorticosteroidsDrugs increasing or potentiating the activity of glucocorticosteroids
10.
POLYMORPHS OF VORINOSTAT AND VORINOSTAT POTASSIUM SALT AND PROCESS FOR PREPARATION THEREOF
Crystalline Vorinostat potassium salt form A characterized by a powder XRD pattern having peaks at about 4.9 and 7.4 ± 0.2 degrees 2-theta and any 3 peaks selected from the lis consisting of: 12.3, 19.8, 20.9, 22.1, 22.8, 28.7 and 29.5 ± 0.2 degrees 2-theta is provided. Crystalline Vorinostat potassium salt form A may be polymorphically pure. Processes for preparing crystalline Vorinostat potassium salt form A are also provided. Further provided i crystalline Vorinostat form VI characterized by a powder XRD pattern having peaks at about 14.3, 14.8, 17.6, 21.4 and 23.1 ± 0.2 degrees 2-theta as well as processes for preparing crystalline Vorinostat form VI.
C07C 239/18 - Hydroxylamino compounds or their ethers or esters having nitrogen atoms of hydroxylamino groups further bound to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
11.
POLYMORPHS OF FLUTICASONE FUROATE AND PROCESS FOR PREPARATION THEREOF
C07J 31/00 - Normal steroids containing one or more sulfur atoms not belonging to a hetero ring
A61K 31/58 - Compounds containing cyclopenta[a]hydrophenanthrene ring systemsDerivatives thereof, e.g. steroids containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin
A61P 5/44 - GlucocorticosteroidsDrugs increasing or potentiating the activity of glucocorticosteroids
12.
CRYSTALLINE FORMS OF ERLOTINIB BASE AND ERLOTINIB HCL
The preparation of crystalline Erlotinib base form G2 is described. This crystalline form can be converted to an Erlotinib salt, such as Erlotinib HCl, which can be used in the treatment of patients with locally advanced or metastatic non-small cell lung cancer (NSCLC).
SALTS OF (R)-5-(2-PHENYLSULPHONYLETHENYL)-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)-lH-indole of the Formula:(I) wherein HX is an acid selected from para-toluene sulfonic acid, benzene sulphonic acid, trifluoroacetic acid, methane sulphonic acid, formic acid and succinic acid; and to processes of preparing and using such salts.
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
C07D 413/04 - Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring- member bond
15.
PROCESSES FOR THE PREPARATION OF CRYSTALLINE FORMS A, B AND PURE CRYSTALLINE FORM A OF ERLOTINIB HCL
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
A61K 31/517 - PyrimidinesHydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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 F(I)
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
20.
AMORPHOUS ELETRIPTAN HYDROBROMIDE AND PROCESS FOR PREPARING IT AND OTHER FORMS OF ELETRIPTAN HYDROBROMIDE
The invention encompasses amorphous elelnptan hydrobromide, processes for preparing it and pharmaceutical compositions of it. The invention also relates to processes for preparing other forms of eletriptan hydrobromide such as Form α and Form β.
C07D 403/06 - Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
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