Sign In to Follow Application
View All Documents & Correspondence

Novel Processes For The Preparation Of Amorphous Linagliptin

Abstract: NOVEL PROCESSES FOR THE PREPARATION OF AMORPHOUS LINAGLIPTIN ABSTRACT The present invention relates to the novel processes for preparation of amorphous Linagliptin. Fig. 01

Get Free WhatsApp Updates!
Notices, Deadlines & Correspondence

Patent Information

Application #
Filing Date
06 January 2021
Publication Number
45/2022
Publication Type
INA
Invention Field
CHEMICAL
Status
Email
docketing@premierip.in
Parent Application
Patent Number
Legal Status
Grant Date
2023-12-22
Renewal Date

Applicants

MOREPEN LABORATORIES LIMITED
Village & P.O.-Masulkhana, Parwanoo, Distt. –Solan, Himachal Pradesh 173220, India (IN)

Inventors

1. SANJAY SURI
Morepen Laboratories Limited Village & P.O.-Masulkhana, Parwanoo, Distt. –Solan, Himachal Pradesh 173220, India (IN)
2. MADAN PAL TANWAR
Morepen Laboratories Limited Village & P.O.-Masulkhana, Parwanoo, Distt. –Solan, Himachal Pradesh 173220, India (IN)
3. SUMAN KUMAR SHARMA
Morepen Laboratories Limited Village & P.O.-Masulkhana, Parwanoo, Distt. –Solan, Himachal Pradesh 173220, India (IN)
4. SANJAY KUMAR MISHRA
Morepen Laboratories Limited Village & P.O.-Masulkhana, Parwanoo, Distt. –Solan, Himachal Pradesh 173220, India (IN)

Specification

FIELD OF THE INVENTION: The present invention primarily discloses novel processes for the preparation of amorphous Linagliptin in a suitable solvent/s using spray drying technique. BACKGROUND OF THE INVENTION: Linagliptin, namely 8-(3R)-3-aminopiperidinyl)-7-butyn-2-yl-3 -methyl-1 -(4- methylquinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione or l-[(4-Methyl-quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-l-yl)-8-(3-(R)-amino- piperidin-1-yl) xanthine, of formula I, is a long acting inhibitor of dipeptidylpeptidase-IV (DPP-IV) activity, at present under development for the treatment of type II diabetes mellitus. Its international non-proprietary name is Linagliptin [CAS number: 668270-12-0] which has the following chemical structure of formula I. Formula I US patent number 7,407,955 (US '955) discloses Linagliptin, related compounds and their pharmaceutical compositions. Further, it describes a process for the preparation of Linagliptin wherein tert-butyloxy carbonyl (Boc) protectedLinagliptin is deprotected using 5-6 M isopropanolic hydrochloric acid or equivalent acid, followed by purification using chromatography. The process disclosed in US '955 is schematically represented in scheme-1. UN DMF,rt, 86<£ o^ KXO_v DMF, n 77-88% 0 rA DTPEA Br » i) racemisation (R)- or (S)-3-Boc-

Documents

Application Documents

# Name Date
1 202111000551-STATEMENT OF UNDERTAKING (FORM 3) [06-01-2021(online)].pdf 2021-01-06
2 202111000551-PROVISIONAL SPECIFICATION [06-01-2021(online)].pdf 2021-01-06
3 202111000551-POWER OF AUTHORITY [06-01-2021(online)].pdf 2021-01-06
4 202111000551-FORM 1 [06-01-2021(online)].pdf 2021-01-06
5 202111000551-DRAWINGS [06-01-2021(online)].pdf 2021-01-06
6 202111000551-DECLARATION OF INVENTORSHIP (FORM 5) [06-01-2021(online)].pdf 2021-01-06
7 202111000551-Proof of Right [08-02-2021(online)].pdf 2021-02-08
8 202111000551-DRAWING [27-12-2021(online)].pdf 2021-12-27
9 202111000551-CORRESPONDENCE-OTHERS [27-12-2021(online)].pdf 2021-12-27
10 202111000551-COMPLETE SPECIFICATION [27-12-2021(online)].pdf 2021-12-27
11 202111000551-FORM 18 [18-02-2022(online)].pdf 2022-02-18
12 202111000551-FER.pdf 2022-11-25
13 202111000551-OTHERS [22-05-2023(online)].pdf 2023-05-22
14 202111000551-FER_SER_REPLY [22-05-2023(online)].pdf 2023-05-22
15 202111000551-CORRESPONDENCE [22-05-2023(online)].pdf 2023-05-22
16 202111000551-US(14)-HearingNotice-(HearingDate-07-12-2023).pdf 2023-11-02
17 202111000551-Correspondence to notify the Controller [02-12-2023(online)].pdf 2023-12-02
18 202111000551-FORM-26 [06-12-2023(online)].pdf 2023-12-06
19 202111000551-Written submissions and relevant documents [14-12-2023(online)].pdf 2023-12-14
20 202111000551-PatentCertificate22-12-2023.pdf 2023-12-22
21 202111000551-IntimationOfGrant22-12-2023.pdf 2023-12-22

Search Strategy

1 SearchreportE_24-11-2022.pdf

ERegister / Renewals

3rd: 14 Mar 2024

From 06/01/2023 - To 06/01/2024

4th: 14 Mar 2024

From 06/01/2024 - To 06/01/2025

5th: 03 Jan 2025

From 06/01/2025 - To 06/01/2026