公开(公告)号：US11059813B2

公开(公告)日：2021-07-13

申请号：US16628746

申请日：2018-07-07

Applicant: BIOCON LIMITED

Inventor： Ramakrishna Parameshwar Bhat ,  Jithendrababu Raghunadhachetty ,  Raghavendracharyulu Venkata Palle ,  Mariappan Kaliappan ,  Reddy VijayBhaskar Regalla

IPC: C07D417/12 ,  C07D417/14

Abstract: The present invention provides for the dasatinib-thymine co-crystal and dasatinib-adenine co-crystal. The present invention further provides dasatinib-butanediol solvate. The present invention further provides for crystalline dasatinib-(±)-1, 2-Butanediol, crystalline dasatinib (R)-1, 2-Butanediol, crystalline dasatinib (S)-1, 2-Butanediol and crystalline dasatinib (±)-2, 3-Butanediol and processes for preparation thereof. The present invention also provides for a process for preparation of amorphous dasatinib using dasatinib-butanediol solvate. The present invention further provides for the preparation of anhydrous dasatinib. The present invention also provides for a process for preparation of dasatinib monohydrate from anhydrous dasatinib.

公开(公告)号：US20180170859A1

公开(公告)日：2018-06-21

申请号：US15736981

申请日：2016-06-16

Applicant: BIOCON LIMITED

Inventor： Venkata Raghavendracharyulu Palle ,  Ramakrishna Parameshwar Bhat ,  Mariappan Kaliappan ,  Jithendra R. Babu ,  Rajmahendra Shanmughasamy

IPC: C07C255/23 ,  C07C253/14 ,  C07D261/08

CPC classification number: C07C255/23 ,  C07C253/00 ,  C07C253/14 ,  C07D261/08 ,  G01N23/20075 ,  G01N25/4866 ,  G01R33/46

Abstract: The present invention provides a process for the preparation of Teriflunomide (Formula-I). The present invention describes the synthesis of Teriflunomide without isolating the intermediate Leflunomide. Teriflunomide is prepared from 5-Methyl isoxazole-4-carboxylic acid by converting to its acid chloride and coupling with 4-trifluoromethyl aniline to obtain Leflunomide (which is not isolated) followed by ring opening reaction using aq. Sodium Hydroxide to form Teriflunomide. In other words, the process is telescoped from 5-methylisoxazole-4-carbonyl chloride.

公开(公告)号：US10526279B2

公开(公告)日：2020-01-07

申请号：US15736981

申请日：2016-06-16

Applicant: BIOCON LIMITED

Inventor： Venkata Raghavendracharyulu Palle ,  Ramakrishna Parameshwar Bhat ,  Mariappan Kaliappan ,  Jithendra R. Babu ,  Rajmahendra Shanmughasamy

IPC: C07C255/23 ,  C07C253/14 ,  C07D261/08 ,  C07C253/00 ,  G01N23/20 ,  G01N25/48 ,  G01R33/46

Abstract: The present invention provides a process for the preparation of Teriflunomide (Formula-I). The present invention describes the synthesis of Teriflunomide without isolating the intermediate Leflunomide. Teriflunomide is prepared from 5-Methyl isoxazole-4-carboxylic acid by converting to its acid chloride and coupling with 4-trifluoromethyl aniline to obtain Leflunomide (which is not isolated) followed by ring opening reaction using aq. Sodium Hydroxide to form Teriflunomide. In other words, the process is telescoped from 5-methylisoxazole-4-carbonyl chloride.