Cariprazine pharmaceutical salt and crystal form, preparation method and application thereof

A technology of cariprazine and medicinal salt, which is applied in the field of cariprazine medicinal salt and its crystal form, preparation and application, which can solve the problems of poor medication compliance of patients, and achieve good market prospect and stable crystal form Good performance and good storage stability

Active Publication Date: 2022-03-18
SHANGHAI BOCIMED PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Currently on the market is Cariprazine Hydrochloride Capsules, which is an oral preparation and requires daily administration to maintain its blood concentration, but due to the need for frequent administration, the patient's medication compliance is poor

Method used

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  • Cariprazine pharmaceutical salt and crystal form, preparation method and application thereof
  • Cariprazine pharmaceutical salt and crystal form, preparation method and application thereof
  • Cariprazine pharmaceutical salt and crystal form, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0142] Embodiment 1: the preparation of cariprazine pamoate

[0143]Dissolve 4000mg (9.36mmol) cariprazine in 200mL (5.4mg / mL) phosphoric acid solution to obtain solution A; dissolve 3634mg (9.36mmol) pamoic acid in 100mL (7.5mg / mL) sodium hydroxide solution In, solution B was obtained. Under stirring, 100 mL of solution B was added to 200 mL of solution A within 30 minutes, the product was separated by filtration and rinsed with water, and vacuum-dried at 40° C. for 12 hours to obtain 5840 mg of a light yellow solid with a yield of 76% (calculated as free base).

[0144] The structure and molar ratio of the cariprazine pamoate described in the present invention are confirmed by proton nuclear magnetic resonance spectrum.

[0145] 1 H-NMR (400MHz, DMSO-d6): δ8.38(s,2H), 8.16(d,2H), 8.80(d,2H), 7.39-7.13(m,7H), 5.86(d,1H), 4.76(s,2H), 3.40-3.32(m,3H), 3.22-3.18(m,4H), 2.75(s,6H), 1.76(t,4H), 1.63-1.57(m,2H), 1.25- 1.16(m,3H), 1.04-0.96(m,2H).

[0146] NMR results showed th...

Embodiment 2

[0148] Example 2: Preparation of Cariprazine Pamoate Amorphous Form

[0149] Under the condition of 60°C, 20g (46.8mmol) cariprazine and 18.17g (46.8mmol) pamoic acid were dissolved in 170mL THF:MeOH (2:1) mixed solvent, filtered, concentrated under reduced pressure to remove the solvent, and then Add 300mL of methanol, dissolve at 60°C, concentrate under reduced pressure to remove the solvent, and dry under vacuum at 40°C for 12 hours to obtain 36.6g of amorphous cariprazine pamoate.

Embodiment 3

[0150] Embodiment 3: Preparation of cariprazine hemipamoate

[0151] Dissolve 200mg (0.468mmol) cariprazine in 10mL (5.4mg / mL) phosphoric acid solution to obtain solution A; dissolve 90.85mg (0.234mmol) pamoic acid in 2.5mL (7.5mg / mL) hydrogenation Sodium solution to obtain solution B. With stirring, 2.5 mL of solution B was added to 10 mL of solution A within 30 minutes, the product was separated by filtration and washed with water, and dried in vacuum at 40° C. for 12 hours to obtain 204 mg of light yellow solid with a yield of 70%.

[0152] The structure and molar ratio of the cariprazine pamoate described in the present invention are confirmed by proton nuclear magnetic resonance spectrum.

[0153] 1 H-NMR (400MHz, DMSO-d6): δ8.25(s,1H), 8.18(d,1H), 7.69(d,1H), 7.38-7.31(m,2H), 7.22-7.14(m,2H ), 7.05(t,1H), 5.86(d,1H), 4.71(s,1H), 3.39-3.22(m,5H), 2.75(s,6H), 1.75(t,4H), 1.59-1.54( m, 2H), 1.25-1.15 (m, 3H), 1.04-0.95 (m, 2H).

[0154] NMR results showed that caripraz...

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Abstract

The invention provides a cariprazine pharmaceutical salt, a preparation method, a pharmaceutical composition containing the cariprazine pharmaceutical salt and application of the cariprazine pharmaceutical salt. The invention discloses a cariprazine medicinal salt. The cariprazine medicinal salt is a salt formed by cariprazine free alkali and an organic acid with more than six carbons. The cariprazine pharmaceutical salt disclosed by the invention is relatively good in solubility and stability and good in market prospect.

Description

[0001] This application claims the priority rights of the following earlier applications: the Chinese invention patent application with the application number 202010870701.6 submitted to the State Intellectual Property Office of China on August 26, 2020; the application submitted to the State Intellectual Property Office of China on August 26, 2020 Chinese Invention Patent Application No. 202010869671.7; Chinese Invention Patent Application No. 202110324874.2 filed with SIPO on March 26, 2021; and 202110330670 filed with SIPO on March 26, 2021 .X's Chinese invention patent application. The entirety of the aforementioned prior application is incorporated herein by reference. technical field [0002] The invention relates to cariprazine medicinal salt and its crystal form, preparation method and application. Background technique [0003] Cariprazine (Formula I) is a novel atypical antipsychotic that has antagonistic effects on dopamine D3, dopamine D2 and serotonin 2B recepto...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/135A61K31/495A61P25/18
CPCA61P25/18A61K9/10A61K31/495A61K47/38A61K47/26A61K47/02C07D295/135A61P25/00Y02A50/30A61K9/14A61K9/0024C07B2200/13
Inventor 应述欢陈志祥张贤朱涛王婷婷刘爽
Owner SHANGHAI BOCIMED PHARMA CO LTD
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