# US 9,518,086 B2 · Crystalline and amorphous forms of a β-arrestin effector > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 9,518,086 B2 - Document ID: US9518086B2 - Status: Granted - Kind: B2 - Application number: 14/616,487 - Filed: 2015-02-06 - Published: 2015-08-13 - Granted: 2016-12-13 - Earliest claimed: 2014-02-07 - Assignees: Trevena, Inc. - Applicants: Trevena, Inc. - Inventors: Ritesh Sanghvi; Gregory Alcorn; Graham Richard Lawton; Meiki Yu; Matthew Ronsheim; Jiaher Tian; Shao Hong Zhou; Yuriy B. Kalyan - Web page: https://patentgrep.com/patent/US9518086B2 ## CPC - C07K 7/64: Cyclic peptides containing only normal peptide links - A61K 38/12: Cyclic peptides {, e.g. bacitracins; Polymyxins; Gramicidins S, C; Tyrocidins A, B or C (A61K38/043 - A61K38/046 take precedence)} - A61P 9/00: Drugs for disorders of the cardiovascular system - A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure - A61P 9/12: Antihypertensives - A61P 13/12: of the kidneys - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - C07K 7/06: having 5 to 11 amino acids - A61K 38/00: Medicinal preparations containing peptides (peptides containing beta-lactam rings A61K31/00; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, A61K31/00; ergot alkaloids of the cyclic peptide type A61K31/48; containing macromolecular compounds having statistically distributed amino acid units A61K31/74; medicinal preparations containing antigens or antibodies A61K39/00; medicinal preparations characterised by the non-active ingredients, e.g. peptides as drug carriers, A61K47/00) - C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00) - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract The present disclosure provides novel crystalline forms of a compound that acts as a β-arrestin effector, processes for preparing novel crystalline and amorphous forms of a compound that acts as a β-arrestin effector and uses thereof. ## Claims ### Claim 1 A crystalline form of a polypeptide having the amino acid sequence SEQ.ID.NO.1, wherein the form is Form I of SEQ.ID.NO.1. ### Claim 2 (depends on 1) The crystalline Form I of claim 1 characterized by an X-ray powder diffraction pattern comprising a peak at about 18.5±0.5 degrees 2θ. ### Claim 3 (depends on 1) The crystalline Form I of claim 1 characterized by an X-ray powder diffraction pattern comprising peaks at about 18.5±0.5 degrees 2θ and at about 10.1±0.5 degrees 2θ. ### Claim 4 (depends on 1) The crystalline Form I of claim 1 characterized by an X-ray powder diffraction pattern comprising peaks: at about 20.2±0.5 degrees 2θ, at about 10.1±0.5 degrees 2θ, and at about 24.4±0.5 degrees 2θ. ### Claim 5 (depends on 1) The crystalline Form I of claim 1 characterized by an X-ray powder diffraction pattern comprising one or more peaks at about 18.5±0.5 degrees 2θ, at about 10.1±0.5 degrees 2θ, at about 8.2±0.5 degrees 2θ, at about 20.2±0.5 degrees 2θ, and at about 24.4±0.5 degrees 2θ. ### Claim 6 (depends on 1) The crystalline Form I of claim 1 characterized by an X-ray powder diffraction pattern comprising one or more peaks as shown in FIG. 4. ### Claim 7 (depends on 1) The crystalline Form I of claim 1 characterized by an X-ray powder diffraction pattern comprising one or more d-spacing values at about 10.7±0.5 degrees angstroms, at about 8.7±0.5 degrees angstroms, at about 4.7±0.5 degrees angstroms, at about 4.1±0.5 degrees angstroms, and at about 3.6±0.5 degrees angstroms. ### Claim 8 (depends on 1) A pharmaceutical composition comprising the crystalline Form I of claim 1. ### Claim 9 (depends on 8) The pharmaceutical composition of claim 8, further comprising an additional drug for the treatment of a cardiovascular or a cardiorenal disorder. ### Claim 10 (depends on 1) The crystalline Form I of claim 1 characterized by an X-ray powder diffraction pattern comprising a peak at about 10.1±0.5 degrees 2θ. ### Claim 11 (depends on 1) The crystalline Form I of claim 1 characterized by an X-ray powder diffraction pattern comprising a peak at about 8.2±0.5 degrees 2θ. ### Claim 12 (depends on 1) The crystalline Form I of claim 1 characterized by an X-ray powder diffraction pattern comprising a peak at about 20.2±0.5 degrees 2θ. ### Claim 13 (depends on 1) The crystalline Form I of claim 1 characterized by an X-ray powder diffraction pattern comprising a peak at about 24.4±0.5 degrees 2θ. ### Claim 14 (depends on 1) The crystalline Form I of claim 1 characterized by an X-ray powder diffraction pattern comprising peaks at about 10.1±0.5±0.5 degrees 2θ and at about 8.2±0.5 degrees 2θ. ### Claim 15 (depends on 1) The crystalline Form I of claim 1 characterized by an X-ray powder diffraction pattern comprising peaks at about 8.2±0.5 degrees 2θ and at about 20.2±0.5 degrees 2θ. ### Claim 16 (depends on 1) The crystalline Form I of claim 1 characterized by an X-ray powder diffraction pattern comprising peaks at about 20.2±0.5 degrees 2θ and at about 10.1±0.5 degrees 2θ. ### Claim 17 (depends on 1) The crystalline Form I of claim 1 characterized by an X-ray powder diffraction pattern comprising peaks at about 20.2±0.5 degrees 2θ and at about 24.4±0.5 degrees 2θ. ### Claim 18 (depends on 1) The crystalline Form I of claim 1 characterized by an X-ray powder diffraction pattern comprising peaks at about 8.2±0.5 degrees 2θ, at about 18.5±0.5 degrees 2θ, and at about 20.2±0.5 degrees 2θ. ### Claim 19 A process for preparing a crystalline form of a polypeptide having an amino acid sequence of SEQ.ID.NO.1, comprising crystallizing SEQ.ID.NO.1 to form Form I of SEQ.ID.NO.1 and optionally isolating the Form I of SEQ.ID.NO.1. ### Claim 20 (depends on 18) The process of claim 18, wherein the crystallizing comprises dissolving a polypeptide having an amino acid sequence of SEQ.ID. NO.1 in an aqueous solution and crystallizing SEQ.ID.NO.1 to form Form I therefrom. ### Claim 21 (depends on 20) The process of claim 20, wherein the aqueous solution is deionized water. ### Claim 22 (depends on 19) The process of claim 19, wherein the aqueous solution consists of deionized water. ### Claim 23 A method of treating a cardiovascular or a cardiorenal disorder comprising administering to a patient in need thereof a crystalline Form I of a polypeptide having an amino acid sequence of SEQ.ID.NO.1. ### Claim 24 (depends on 23) The method of claim 23, wherein the cardiovascular or the cardiorenal disorder is heart failure. ### Claim 25 (depends on 23) The method of claim 23, wherein the patient has been diagnosed with heart failure.