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“Solid Forms Of Venetoclax”

Abstract: The present invention relates to the process for preparing solid forms of 4-(4-{[2-(4-chlorophenyl)-4,4dimethylcyclohex-1 -en-1 -yl] methyl} piperazin-1 -yl)-N-( { 3 -nitro-4-[(tetrahydro-2H-pyran-4ylmethyl) amino] phenyl} sulfonyl)-2-(lH-pyrrolo[2,3-B] pyridin-5-yloxy) benzamide) (Venetoclax)

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Notices, Deadlines & Correspondence

Patent Information

Application #
Filing Date
19 September 2018
Publication Number
12/2020
Publication Type
INA
Invention Field
CHEMICAL
Status
Email
radha@biophore.com
Parent Application

Applicants

Biophore India pharmaceuticals Pvt. Ltd
Plot#92; 1-98/2/92, Kavuri Hills – Phase II, Jubilee Hills, Hyderabad

Inventors

1. Manik Reddy Pullagurla
Plot#92; 1-98/2/92, Kavuri Hills – Phase II, Jubilee Hills, Hyderabad, 500033.
2. Bhaskar Reddy Pitta
Plot#92; 1-98/2/92, Kavuri Hills – Phase II, Jubilee Hills, Hyderabad, 500033.
3. Rajesham Boge
Plot#92; 1-98/2/92, Kavuri Hills – Phase II, Jubilee Hills, Hyderabad, 500033.
4. Jagadeesh Babu Rangisetty
Plot#92; 1-98/2/92, Kavuri Hills – Phase II, Jubilee Hills, Hyderabad, 500033.

Specification

We Claim:
1. A process for preparing crystalline forms Bl, B2, B3, B4, B5, B6, B7 and B8
of Venetoclax (1), comprising of the following steps:
a) Providing Venetoclax (1) in a suitable protic or aprotic solvent or mixtures;
b) heating the reaction mixture at a suitable temperature;
c) optionally, filtering and adding a suitable aprotic solvent;
d) cooling the reaction mixture to a suitable temperature; and
e) isolating crystalline forms of Venetoclax (1).
2. A process for preparing amorphous form of Venetoclax (1) comprising:
a) Providing Venetoclax (1) in a suitable protic or aprotic solvent or mixtures thereof;
b) stirring the reaction mixture and filtering C;
c) heating the reaction mixture at a suitable temperature;
d) cooling the reaction mixture to a suitable temperature; and
e) isolating amorphous forms of Venetoclax (1).
3. A process for the preparing solid dispersions of Venetoclax (1) comprising:
a) Providing Venetoclax (1) in a suitable aprotic solvent;
b) adding ta suitable pharmaceutically acceptable excipients at a suitable temperature;
c) stirring the reaction mixture;
d) isolating amorphous solid dispersion of Venetoclax (1); and
e) drying under suitable conditions.
4. The process of claim 3, wherein the suitable pharmaceutically acceptable
excipients used herein is selected from a group comprising of lactose, sorbitol,
mannitol, saccharose, cellulose, methyl cellulose, ethyl cellulose,
microcrystalline cellulose, polyethylene glycol (PEG), polyvinylpyrrolidone
(PVP), polyvinylpyrrolidone K-30, (PVP K-30), polyvinyl acetate

hydroxyethyl cellulose (HEC), hydroxy propyl methyl cellulose (HPMC), hydroxypropyl cellulose (HPC), hydroxy propyl methyl cellulose acetate succinate (HPMC-AS), Y-cyclodextrin, hydroxypropyl beta cyclodextrin (HPBCD), sulfobutylether-(3-cyclodextrin (SBCED).
5. The process of claim 1 and claim 2, wherein the suitable protic solvent used is selected from a group comprising of water, methanol, ethanol, ethylene glycol, isopropyl alcohol, benzyl alcohol or mixtures thereof.
6. The process of claim 1 , claim 2 and claim 3, wherein the suitable aprotic solvent used herein is selected from a group comprising of acetone, methyl ethyl ketone , acetonitrile, nitromefhane, 1,4-dioxane, diethyl ether, dichloromethane, ethyl acetate, isopropyl acetate, n-butyl acetate, N, N-dimethylformamide, N,N-dimethyl acetamide, methyl tertiary butyl ether, hexane, cyclohexane, n-heptane, toulene, xylene, tetrahydrofuran or mixtures thereof.
7. The process of claim 1, claim 2 and claim 3, wherein the suitable drying condition used herein is selected from a group comprising of drying, using an air tray dryer, vacuum tray dryer, fluidized bed dryer, spin flash dryer, flash dryer and spray dryer.

8. The process of claim 1, wherein the crystalline form B2 of Venetoclax (1) is isolated as toluene solvate.
9. The process of claim 1, wherein the crystalline form B3 of Venetoclax (1) is isolated as anhydrate with moisture content less than 2%(w/w).

Documents

Application Documents

# Name Date
1 201841035315-PROVISIONAL SPECIFICATION [19-09-2018(online)].pdf 2018-09-19
2 201841035315-FORM 1 [19-09-2018(online)].pdf 2018-09-19
3 201841035315-DRAWINGS [19-09-2018(online)].pdf 2018-09-19
4 Form1_After Filed_05-10-2018.pdf 2018-10-05
5 Correspondence by Applicant_Form1_05-10-2018.pdf 2018-10-05
6 201841035315-FORM FOR SMALL ENTITY [16-09-2019(online)].pdf 2019-09-16
7 201841035315-FORM 3 [16-09-2019(online)].pdf 2019-09-16
8 201841035315-EVIDENCE FOR REGISTRATION UNDER SSI [16-09-2019(online)].pdf 2019-09-16
9 201841035315-ENDORSEMENT BY INVENTORS [16-09-2019(online)].pdf 2019-09-16
10 201841035315-DRAWING [16-09-2019(online)].pdf 2019-09-16
11 201841035315-COMPLETE SPECIFICATION [16-09-2019(online)].pdf 2019-09-16
12 Correspondence by Agent_Power of Attorney_30-09-2019.pdf 2019-09-30