Abstract: The present invention provides a crystalline Form I of afatinib dimaleate, its process for preparation and pharmaceutical composition thereof, and its use in the treatment of metastatic non-small cell lung cancer.

Abstract: The present invention provides a crystalline form of baricitinib characterized by an XRPD pattern substantially as depicted in FIG. 1, a process for its preparation, a pharmaceutical composition comprising it, and its use for the treatment of JAK-associated diseases.

Abstract: The present invention provides a process for the preparation of baricitinib and an intermediate thereof. The present invention provides a convenient, economical, and industrially advantageous two-step process for the preparation of [4-(IH-pyrazol-4-yl)-7Hpyrrolo[2,3-d] pyrimidin-7-yl]methyl pivalate of Formula (II). The process of the present invention involves the use of an alkali or alkaline earth metal hydroxide, carbonate, or bicarbonate as a base for reacting 4-chloro-7H-pyrrolo[2,3-d]pyrimidine of Formula (III) with chloromethyl pivalate of Formula (IV), and the use of an unprotected pyrazole borolane of Formula (VIII) for the conversion of (4-chloro-7H-pyrrolo[2,3-d] pyrimidin-7-yl)methyl 2,2-dimethylpropanoate of Formula V into [4-(1H-pyrazol-4-yl)-7Hpyrrolo[2,3-d]pyrimidin-7-yl]methyl pivalate of Formula (II). The process of the present invention provides [4-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]methyl pivalate of Formula (I) in high yield.

Abstract: The present invention relates to processes for the preparation of ertugliflozni. The present invention also provides compounds of Formula (III), Formula (IV), and Formula (VII), processes for their preparation, and their use for the preparation of ertugliflozin. The processes of the present invention involve protecting the ertugliflozin intermediate compound with a suitable protecting group which provides ertugliflozin having high purity and yield.

Abstract: The present invention provides a process for the preparation of baricitinib and an intermediate thereof. The present invention provides a convenient, economical, and industrially advantageous two-step process for the preparation of [4-(IH-pyrazol-4-yl)-7Hpyrrolo[2,3-d] pyrimidin-7-yl]methyl pivalate of Formula (II). The process of the present invention involves the use of an alkali or alkaline earth metal hydroxide, carbonate, or bicarbonate as a base for reacting 4-chloro-7H-pyrrolo[2,3-d]pyrimidine of Formula (III) with chloromethyl pivalate of Formula (IV), and the use of an unprotected pyrazole borolane of Formula (VIII) for the conversion of (4-chloro-7H-pyrrolo[2,3-d] pynmidin-7-yl)methyl 2,2-dimethylpropanoate of Formula V into [4-(1H-pyrazol-4-yl)-7Hpyrrolo[2,3-d]pyrimidin-7-yl]methyl pivalate of Formula (II). The process of the present invention provides [4-(1H-pyrazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl]methyl pivalate of Formula (I) in high yield.

Abstract: The present invention provides processes for the preparation of ibrutinib, intermediate compounds of Formula VI and Formula VIII, and salts thereof. The processes of the present invention are commercially viable, cost-effective, environmentally friendly, and make use of inexpensive, non-hazardous, safe chemicals that are easy to handle.

Abstract: The present invention provides a process for the preparation of pazopanib of Formula Ia or salts, and intermediates thereof.

Abstract: Provided are methods to destabilize emulsion feedstocks. Benefits of the provided methods include a reducing or eliminating the amount of acid necessary to process the feedstocks, less processing time, cleaner separation of the resulting phases, and increased recovery of valuable products. In the methods, a moderate temperature is applied to the feedstock to create a first mixture. The moderate temperature may be between 120 and 220 degrees Celsius. The first mixture is mixed at the moderate temperature, such as by staged mixing in some embodiments. Moreover, the first mixture is retained at the moderate temperature for up to six hours. The first mixture is separated into an oil phase, convoluted phase, and a water phase. In some embodiments, the moderate temperature may be 125 to 150 degrees Celsius, such as between 125 and 130 degrees Celsius. Moreover, the first mixture may be retained at the moderate temperature for between forty-five minutes and four hours, such as from two to four hours.

Abstract: The present invention provides a stable topical pharmaceutical composition of halobetasol propionate. The present invention discloses an impurity of compound of Formula II and its process of preparation. It also relates to a method of evaluating stability of a topical pharmaceutical composition of halobetasol propionate.

Abstract: The present invention provides a process for the preparation of 4-dimethylaminocrotonic acid of Formula (II) or its salts, which is used as an intermediate for the preparation of afatinib or its salts.

Abstract: Methods for producing oil from fats and oils having high free fatty acid content are provided. In the method, fats and oils are treated with a mixture including an alcohol to result in a low-free fatty acid oily phase and an alcohol phase. The mixture may also include an alkali. The alcohol may be a monohydric alcohol and an aqueous alcohol, such as an aqueous alcohol having a concentration of at least about 15% alcohol-by-weight. The low-free fatty acid phase may include oil and at least one impurity. The low-free fatty acid phase may be cooled, and the oil may be separated from the at least one impurity. Fats and oils amenable to such a method may include, but are not limited to, waste fats, waste oils, high acid grease, high acid tallow, sorghum heat oil, and corn oil, such as corn oil produced at an ethanol production plant.

Abstract: The present invention relates to a stable amorphous ticagrelor and a process for its preparation.

Abstract: The present invention provides a crystalline Form I of afatinib dimaleate, its process for preparation and pharmaceutical composition thereof, and its use in the treatment of metastatic non-small cell lung cancer.

Abstract: The present invention provides crystalline Form I, Form II, Form III, Form IV, Form V, Form V-A, Form VI, Form VII, and Form VIII of palbociclib, processes for their preparation, pharmaceutical compositions comprising these crystalline forms, and their use for the treatment of cyclin-dependent kinase associated diseases.

Abstract: The present invention relates to a process for the preparation of palbociclib utilizing a silyl-protected crotonic acid derivative to produce a silyl-protected 2-chloro-4-(cyclopentylamino)-5-(1-methyl-2-carboxy-ethen-1-yl)pyrmidine followed by intramolecular cyclization of the pyrmidine intermediate to produce 2-chloro-8-cyclopentyl-5-methyl-8H-pyrido[2,3-d]pyrimidin-7-one which is then converted to palbociclib.

Abstract: The present invention provides a crystalline form of baricitinib characterized by an XRPD pattern substantially as depicted in FIG. 1, a process for its preparation, a pharmaceutical composition comprising it, and its use for the treatment of JAK-associated diseases.

Abstract: The present invention relates to a dapagliflozin-citric acid co-crystal, processes for its preparation, and its use for the treatment of type 2 diabetes mellitus. A dapagliflozin citric acid co-crystal. The dapagliflozin citric acid co-crystal of claim 1, characterized by X-ray powder diffraction peaks having d-spacing values at about 3.89, 3.90, 4.01, 4.35, 5.77, and 5.80.

Abstract: The present invention relates to a dapagliflozin-citric acid co-crystal, processes for its preparation, and its use for the treatment of type 2 diabetes mellitus. A dapagliflozin citric acid co-crystal. The dapagliflozin citric acid co-crystal of claim 1, characterized by X-ray powder diffraction peaks having d-spacing values at about 3.89, 3.90, 4.01, 4.35, 5.77, and 5.80.

Abstract: The present invention provides an amorphous form of baricitinib, processes for its preparation, a pharmaceutical composition comprising it, and its use for the treatment of JAK-associated diseases.

Abstract: The present invention provides a process for the preparation of 4-dimethylaminocrotonic acid of Formula (II) or its salts, which is used as an intermediate for the preparation of afatinib or its salts.