Abstract: An improved process for the preparation of key intermediates for tazarotene, 4,4-dimethyl-6-ethynylthiochroman, is provided comprising (a) reacting 4,4-dimethyl-6-acetylthiochroman of the formula with an acid chloride and an amido-group containing compound of the general formula wherein R is hydrogen or a hydrocarbyl of from 1 to 15 carbon atoms and R1 and R2 can be the same or different and are hydrocarbyls of from 1 to 15 carbon atoms or R1 and R2 together with the nitrogen atom to which they are bonded are joined together to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms, or one of R1 and R2 together with the nitrogen atom to which it bonded are joined together with the carbonyl radical to form a heterocyclic group, optionally containing one or more additional heterocyclic atoms to form a ?-chloro vinyl carbonyl compound intermediate of the general formula wherein R has the aforestated meanings; and (b) reacting the ?-chloro vinyl carbonyl compound
Abstract: The present invention provides Stearoyl CoA Desaturase (SCD) inhibitors. In particular, compounds described herein are useful for treating or preventing diseases, conditions and/or disorders modulated by Stearoyl CoA Desaturase 1 (SCD1) inhibitors. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders modulated by Stearoyl CoA Desaturase (SCD) inhibitors.
Abstract: The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.
Abstract: The present invention relates to novel tricyclic compounds useful for the treatment of inflammatory conditions, diseases of the central nervous and insulin resistant diabetes.
Type:
Application
Filed:
June 27, 2007
Publication date:
June 19, 2008
Applicant:
GLENMARK PHARMACEUTICALS S.A.
Inventors:
Gopalan Balasubramanian, Laxmikant A. Gharat, Aftab D. Lakdawala, Raghu R. Anupindi
Abstract: The present invention relates to novel heterocyclic compounds, their analogs, their tautomers, their regioisomers, their stereoisomers, their enantiomers, their diastereomers, their polymorphs, their pharmaceutically acceptable salts, their appropriate N-oxides, their pharmaceutically acceptable solvates and their pharmaceutical compositions containing them. The present invention more particularly relates to novel Phosphodiesterase type 4 (PDE4) inhibitors of the Formula (1), their analogs, tautomers, enantiomers, diasteromers, regioisomers, stereoisomers, polymorphs, pharmaceutically acceptable salts, appropriate N-oxide, pharmaceutically acceptable solvates and the pharmaceutical compositions containing them.
Abstract: Stable pharmaceutical compositions for oral administration are provided comprising an anti-allergic effective amount of descarbonylethoxy-loratadine or a pharmaceutically acceptable salt thereof, a lactose-based excipient and a pharmaceutically acceptable filler wherein the composition is substantially free of a pharmaceutically acceptable basic salt and wherein the composition contains less than about 1% by weight of N-formyl descarbonylethoxyloratadine after storage at a temperature of from about 25° C. to about 40° C. and a relative humidity of about 60% to about 75% for at least 1 month.
Type:
Application
Filed:
October 20, 2006
Publication date:
May 22, 2008
Applicant:
Glenmark Pharmaceuticals Limited
Inventors:
Anandi Krishnan, Arra Ganga Srinivas, Deepika V. Bhat Tamragouri
Abstract: Pharmaceutical compositions suitable for the treatment of skin disorder are provided which include at least a therapeutically effective amount of at least on antiacne agent and at least one antibiotic agent as active pharmaceutical ingredients and a hydrophilic matrix capable of providing a constant and uniform release of the active pharmaceutical ingredients.
Abstract: The present invention relates to novel processes for preparing DPP-IV inhibitors having the structure of formula I, and pharmaceutically acceptable salt thereof, which are useful for treatment of Type 2 diabetes.
Abstract: A process for preparing perindopril is provided comprising condensing an N-[(S)-1-carbethoxybutyl]-(S)-alanyl halide of formula II: wherein X is a halide with an (2S,3aS,7aS)-2-carboxyperhydroindole of formula III: wherein R is hydrogen or a protecting group.
Abstract: Eprosartan mesylate substantially in an amorphous form is disclosed. A composition comprising eprosartan mesylate in a solid form, wherein at least about 80% by weight of the solid eprosartan mesylate is in an amorphous form is also disclosed. The present invention also provides a process for preparing eprosartan mesylate substantially in an amorphous form by providing a solution of eprosartan mesylate in one or more solvents capable of dissolving the eprosartan mesylate and substantially removing the solvent from the solution.
Type:
Application
Filed:
July 17, 2007
Publication date:
January 17, 2008
Applicant:
Glenmark Pharmaceuticals Limited
Inventors:
Anthony Crasto, Samir Naik, Narendra Joshi, Mubeen Khan
Abstract: Pregabalin substantially in an amorphous form is disclosed. A composition comprising amorphous pregabalin in a solid form, wherein at least about 80% by weight of the solid is amorphous pregabalin in an amorphous form is also disclosed. The present invention also provides a process for preparing amorphous pregabalin substantially in an amorphous form by providing a solution of amorphous pregabalin in one or more solvents capable of dissolving the pregabalin and substantially removing the solvent from the solution.
Abstract: Frovatriptan succinate substantially in an amorphous form is disclosed. Also disclosed is a composition comprising frovatriptan succinate in a solid form, wherein at least about 80% by weight of the solid is frovatriptan succinate in an amorphous form. The present invention also provides a process for preparing frovatriptan succinate substantially in an amorphous form by providing a solution of frovatriptan succinate in one or more solvents capable of dissolving the frovatriptan succinate and substantially removing the solvent from the solution.
Type:
Application
Filed:
June 27, 2007
Publication date:
December 27, 2007
Applicant:
Glenmark Pharmaceuticals Limited
Inventors:
Samir Naik, Anthony Crasto, Narendra Joshi, Sachin Srivastava
Abstract: An improved process for the preparation of pyrimidine derivatives is provided comprising reacting a Wittig reagent of the general formula wherein R is an alkyl of from 1 to 10 carbon atoms, aryl or arylalkyl, R1 is a substituted or unsubstituted hydrocarbon group, R2 and R3 are the same or different and are hydrogen or a substituted or unsubstituted hydrocarbon group; Z is sulfur, oxygen, sulfonyl, or imino which may be substituted by formyl, acetyl, propionyl, butyryl, isobutyryl, valeryl, isovaleryl, amino substituted by sulfonyl or alkylsulfonyl, and sulfonyl substituted by alkyl, amino or alkylamino and X is a halogen; with an aldehyde of the general formula wherein R4 is hydrogen, a lower alkyl or a cation capable of forming a non-toxic pharmaceutically acceptable salt and each R5 are the same or different and are hydrogen or a hydrolyzable protecting group, or each R5, together with the oxygen atom to which each is bonded, form a hydrolyzable cyclic protecting group, or each R5 is bonded to the
Abstract: Pharmaceutical compositions containing ezetimibe or its pharmaceutically acceptable salt that is substantially free of microcrystalline cellulose or crystalline cellulose are disclosed. Also disclosed are pharmaceutical compositions containing micronized particles of ezetimibe.
Abstract: A process for preparing perindopril is provided comprising condensing an N-[(S)-1-carbethoxybutyl]-(S)-alanyl halide of formula II: wherein X is a halide with an (2S,3aS,7aS)-2-carboxyperhydroindole of formula III: wherein R is hydrogen or a protecting group.
Abstract: Ropinirole hydrochloride substantially free of impurities and a process for its preparation is provided. Also provided is ropinirole base substantially in polymorph Form A and a process for its preparation. Pharmaceutical compositions containing the same are also provided.
Abstract: The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: wherein X, Y, a, R1, and R2 are as defined herein.
Type:
Application
Filed:
February 15, 2007
Publication date:
October 11, 2007
Applicant:
GLENMARK PHARMACEUTICALS S.A.
Inventors:
Abraham Thomas, Gopalan Balasubramanian, V.S. Lingam, Daisy Shah
Abstract: The present invention provides a novel intermediate of ethyl 6-[2-(4,4-dimethylthiochroman-6-yl)ethynyl] nicotinate or a pharmaceutically acceptable salt thereof and a process for its preparation. The present invention also provides for the preparation of ethyl 6-[2-(4,4-dimethylthiochroman-6-yl)ethynyl] nicotinate of Formula I or a pharmaceutically acceptable salt thereof using the intermediate.
Abstract: The present invention relates to novel compounds useful as dipeptidyl peptidase IV (DPP-IV) inhibitors of the formula: wherein X, Y, a, R1, and R2 are as defined herein.
Type:
Application
Filed:
February 15, 2007
Publication date:
October 4, 2007
Applicant:
GLENMARK PHARMACEUTICALS S.A.
Inventors:
Abraham Thomas, Gopalan Balasubramanian, V.S. Lingam, Daisy Shah