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公开(公告)号：US09822145B2
公开(公告)日：2017-11-21
申请号：US15228689
申请日：2016-08-04
Applicant: Apicore US LLC
Inventor： Ravishanker Kovi , Jayaraman Kannapan , Vasanthakumar G Ramu , Alaparthi Lakshmi Prasad , Talluri Bhushaiah Chowdary , Gaurav Kulkarni , Saiyed Akeel Ahmed Shakeel Ahmed , Veerabhadra Rao Bobbili , N V Raghavalu Dusanapudi , Anand V. Mantri
CPC classification number: C07K5/1016 , C07K5/06078
Abstract: Racemization-free methods are disclosed for the synthesis of carfilzomib. Novel intermediates and methods of making carfilzomib employing fragment condensation using the novel intermediates are disclosed. Amorphous carfilzomib and methods of making same are disclosed.
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公开(公告)号：US10221184B2
公开(公告)日：2019-03-05
申请号：US15862355
申请日：2018-01-04
Applicant: Apicore US LLC
Inventor： Ravishanker Kovi , Jayaraman Kannapan , Ananda Babu Thirunavakarasu , Gaurav Yadav , Veerabhadra Rao Bobbili , Shivnath Sahebrao Patil , Sanjay F. Thakor
IPC: C07D487/04 , A61K31/5025 , B01D9/00
Abstract: Novel crystalline ponatinib hydrochloride forms designated Form alpha and Form beta are disclosed. Form alpha is characterized by data selected from an XRPD pattern with peaks at about 6.5, 9.0, 12.25, 14.4, 16.70, 19.6, 22.2, 24.5, 28.2±0.2 degrees 2-theta; an XRPD pattern substantially as depicted in FIG. 1; and/or a combination thereof. Form beta is characterized by data selected from an XRPD pattern with peaks at about 10.7, 15.2, 15.8, 16.4 23.1, 25.0, 27.8±0.2 degrees 2-theta; an XRPD pattern substantially as depicted in FIG. 3; and/or combinations thereof. Processes for making Form alpha and Form beta are disclosed.
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公开(公告)号：US20160340388A1
公开(公告)日：2016-11-24
申请号：US15228689
申请日：2016-08-04
Applicant: Apicore US LLC
Inventor： Ravishanker Kovi , Jayaraman Kannapan , Vasanthakumar G Ramu , Alaparthi Lakshmi Prasad , Talluri Bhushaiah Chowdary , Gaurav Kulkarni , Saiyed Akeel Ahmed Shakeel Ahmed , Veerabhadra Rao Bobbili , N V Raghavalu Dusanapudi , Anand V. Mantri
CPC classification number: C07K5/1016 , C07K5/06078
Abstract: Racemization-free methods are disclosed for the synthesis of carfilzomib. Novel intermediates and methods of making carfilzomib employing fragment condensation using the novel intermediates are disclosed. Amorphous carfilzomib and methods of making same are disclosed.
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4.发明申请公开(公告)号：US20190002421A1
公开(公告)日：2019-01-03
申请号：US15854458
申请日：2017-12-26
Applicant: Apicore US LLC
Inventor： Ravishanker Kovi , Jayaraman Rao Kannapan , Ananda Babu Thirunavakarasu , Veerabhadra Rao Bobbili , Gaurav Yadav
IPC: C07D295/096
CPC classification number: C07D295/096 , A61K31/496 , C07B2200/13
Abstract: Processes are disclosed for making vortioxetine and pharmaceutically acceptable salts thereof. A propylene glycol solvate of vortioxetine hydrobromide is disclosed. A novel crystalline form of vortioxetine hydrobromide propylene glycol solvate, designated form AC1, is disclosed along with a method for making same. Form AC1 may be characterized by an x-ray powder diffraction pattern with peaks at about 19.64, 22.85, 25.51, 29.57, 30.18±0.2 degrees 2-theta.
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Patent Agency Ranking
公开(公告)号：US20160115198A1
公开(公告)日：2016-04-28
申请号：US14923068
申请日：2015-10-26
Applicant: Apicore US LLC
Inventor： Ravishanker Kovi , Jayaraman Kannapan , Vasanthakumar G Ramu , Alaparthi Lakshmi Prasad , Talluri Bhushaiah Chowdary , Gaurav Kulkarni , Saiyed Akeel Ahmed Shakeel Ahmed , Veerabhadra Rao Bobbili , N V Raghavalu Dusanapudi , Anand V. Mantri
CPC classification number: C07K5/1016 , C07K5/06078
Abstract: Racemization-free methods are disclosed for the synthesis of carfilzomib. Novel intermediates and methods of making carfilzomib employing fragment condensation using the novel intermediates are disclosed. Amorphous carfilzomib and methods of making same are disclosed.
Abstract translation: 公开了不含外消旋化的方法用于合成carfilzomib。 公开了使用新型中间体制备carfilzomib采用片段缩合的新型中间体和方法。 公开了无定形carfilzomib及其制备方法。
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6.发明授权公开(公告)号：US10519121B2
公开(公告)日：2019-12-31
申请号：US15854458
申请日：2017-12-26
Applicant: Apicore US LLC
Inventor： Ravishanker Kovi , Jayaraman Rao Kannapan , Ananda Babu Thirunavakarasu , Veerabhadra Rao Bobbili , Gaurav Yadav
IPC: C07D295/096 , A61K31/496
Abstract: Processes are disclosed for making vortioxetine and pharmaceutically acceptable salts thereof. A propylene glycol solvate of vortioxetine hydrobromide is disclosed. A novel crystalline form of vortioxetine hydrobromide propylene glycol solvate, designated form AC1, is disclosed along with a method for making same. Form AC1 may be characterized by an x-ray powder diffraction pattern with peaks at about 19.64, 22.85, 25.51, 29.57, 30.18±0.2 degrees 2-theta.
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公开(公告)号：US20180208599A1
公开(公告)日：2018-07-26
申请号：US15862355
申请日：2018-01-04
Applicant: Apicore US LLC
Inventor： Ravishanker Kovi , Jayaraman Kannapan , Ananda Babu Thirunavakarasu , Gaurav Yadav , Veerabhadra Rao Bobbili , Shivnath Sahebrao Patil , Sanjay F. Thakor
IPC: C07D487/04 , B01D9/00
CPC classification number: C07D487/04 , B01D9/0036 , B01D9/005 , C07B2200/13
Abstract: Novel crystalline ponatinib hydrochloride forms designated Form alpha and Form beta are disclosed. Form alpha is characterized by data selected from an XRPD pattern with peaks at about 6.5, 9.0, 12.25, 14.4, 16.70, 19.6, 22.2, 24.5, 28.2±0.2 degrees 2-theta; an XRPD pattern substantially as depicted in FIG. 1; and/or a combination thereof. Form beta is characterized by data selected from an XRPD pattern with peaks at about 10.7,15.2, 15.8, 16.4 23.1, 25.0, 27.8±0.2 degrees 2-theta; an XRPD pattern substantially as depicted in FIG. 3; and/or combinations thereof. Processes for making Form alpha and Form beta are disclosed.
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公开(公告)号：US20180037606A1
公开(公告)日：2018-02-08
申请号：US15785966
申请日：2017-10-17
Applicant: Apicore US LLC
Inventor： Ravishanker Kovi , Jayaraman Kannapan , Vasanthakumar G. Ramu , Alaparthi Lakshmi Prasad , Talluri Bhushaiah Chowdary , Gaurav Kulkarni , Saiyed Akeel Ahmed Shakeel Ahmed , Veerabhadra Rao Bobbili , N V Raghavalu Dusanapudi , Anand V. Mantri
CPC classification number: C07K5/1016 , C07K5/06078
Abstract: Racemization-free methods are disclosed for the synthesis of carfilzomib. Novel intermediates and methods of making carfilzomib employing fragment condensation using the novel intermediates are disclosed. Amorphous carfilzomib and methods of making same are disclosed.
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公开(公告)号：US20170260157A1
公开(公告)日：2017-09-14
申请号：US15452444
申请日：2017-03-07
Applicant: Apicore US LLC
Inventor： Ravishanker Kovi , Veerabhadra Rao Bobbili , Jayaraman Kannapan
IPC: C07D401/04
CPC classification number: C07D401/04
Abstract: Processes are disclosed for making pomalidomide which involve reducing 2-(2,6-dioxopiperidin-3-yl)-4-nitroisoindoline-1,3-dione using a catalyst and at least one solvent. The process may include reacting 3-nitrophthalic anhydride with α-amino glutarimide hydrochloride to obtain the 2-(2,6-dioxopiperidin-3-yl)-4-nitroisoindoline-1,3-dione. The process may further include, prior to the reducing step, subjecting the 2-(2,6-dioxopiperidin-3-yl)-4-nitroisoindoline-1,3-dione to a purification process comprising heating a mixture of 2-(2,6-dioxopiperidin-3-yl)-4-nitroisoindoline-1,3-dione and 1,4-dioxane to obtain a solution, treating the obtained solution with carbon, removing the carbon from the solution to obtain a purified 2-(2,6-dioxopiperidin-3-yl)-4-nitroisoindoline-1,3-dione solution and using the purified 2-(2,6-dioxopiperidin-3-yl)-4-nitroisoindoline-1,3-dione solution for the reducing step. Processes disclosed achieve pomalidomide having a purity of greater than 99% as measured by HPLC with no individual impurity present in an amount greater than 0.1% and total impurities comprising not more than 0.5%.
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