# US 11,111,250 B2 · Polymorphs of Ribociclib mono succinate

> Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt

- Number: US 11,111,250 B2
- Document ID: US11111250B2
- Status: Granted
- Kind: B2
- Application number: 16/955,823
- Filed: 2018-12-20
- Published: 2020-10-29
- Granted: 2021-09-07
- Earliest claimed: 2017-12-22
- Assignees: Shilpa Meicare Limited
- Applicants: Shilpa Medicare Limited
- Inventors: Sriram Rampalli; Lav Kumar Upalla; Suryanarayan Cherukuvada; Chanti Babu Patneedi; Gopala Krishna Dasari; Vijaya Murali Mohan Rao Seshagiri
- Web page: https://patentgrep.com/patent/US11111250B2

## CPC

- C07D 487/04: Ortho-condensed systems
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

The present invention relates to novel crystalline and amorphous polymorphic forms of Ribociclib(1) mono succinate. (I) Said crystalline forms may be useful in the improved preparation of oral dosage forms for the treatment of cancer.

## Claims

### Claim 1

Crystalline Ribociclib mono succinate Form-SRS-I characterized by X-ray powder diffraction pattern comprising characteristic 2θ° peaks at 9.0, 13.0, 15.2, 16.5, 17.3, 18.3, 20.0, 21.4, 21.6, 22.1, 23.6, 23.9 and 28.0±0.2 2θ°.

### Claim 2 (depends on 1)

Crystalline Ribociclib mono succinate Form-SRS-I according to claim 1, further characterized by X-ray powder diffraction pattern comprising at 2θ° peaks selected from 4.8, 10.7, 13.5, 14.2, 16.2, 18.0, 19.2, 20.9, 22.7, 23.1, 24.4, 25.4, 26.2, 26.7 and 28.4±0.2 20°.

### Claim 3 (depends on 1)

Crystalline Ribociclib mono succinate Form-SRS-I according to claim 1, further characterized by DSC isotherm comprising endothermic peaks ranging between 175 to 185° C.

### Claim 4

Crystalline Ribociclib mono succinate Form-SRS-I characterized by X-ray powder diffraction pattern comprising characteristic 2θ° peaks at 9.0, 13.0, 15.2, 16.5, 17.3, 18.3, 20.0, 21.4, 21.6, 22.1, 23.6, 23.9 and 28.0±0.2 2θ°, wherein the process for the preparation of Crystalline Ribociclib mono succinate Form-SRS-I comprises the steps of:
a) dissolving succinic acid in first solvent;
b) adding Ribociclib;
c) concentrating the reaction mass;
d) optionally adding second solvent followed by distillation; and
e) isolate the crystalline Ribociclib mono succinate.

### Claim 5 (depends on 4)

Crystalline Ribociclib mono succinate Form-SRS-I according to claim 4, wherein solvent used in step (a) is selected from C1-5-alcohols or Methoxy ethanol, ethoxy methanol or C3-6 Ketones or C1-8 alkanes or dimethyl formamide or dimethyl acetamide or N-methyl pyrrolidine or halogenated organic solvents or Ethers or sulphoxides or esters or water or mixtures thereof.

### Claim 6 (depends on 4)

Crystalline Ribociclib mono succinate Form-SRS-I according to claim 4, wherein solvent used in step (d) is selected from C1-5-alcohols or Methoxy ethanol, ethoxy methanol or C3-6 Ketones or C1-8 alkanes or dimethyl formamide or dimethyl acetamide or N-methyl pyrrolidine or halogenated organic solvents or Ethers or sulphoxides or esters or water or mixtures thereof.