# US 10,765,693 B2 · Polymorphic compounds and uses thereof

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- Number: US 10,765,693 B2
- Document ID: US10765693B2
- Status: Granted
- Kind: B2
- Application number: 16/583,570
- Filed: 2019-09-26
- Published: 2020-03-26
- Granted: 2020-09-08
- Earliest claimed: 2018-09-26
- Assignees: Astrocyte Pharmaceuticals, Inc.
- Applicants: Astrocyte Pharmaceuticals, Inc.
- Inventors: Russell Birch Poe; David T. Jonaitis; Lisa Michelle Grove
- Web page: https://patentgrep.com/patent/US10765693B2

## CPC

- A61K 31/7076: containing purines, e.g. adenosine, adenylic acid
- A61K 31/52: Purines, e.g. adenine
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- C07D 473/24: one nitrogen and one sulfur atom
- C07H 19/16: Purine radicals
- C07B 2200/13: Crystalline forms, e.g. polymorphs
- 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
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- C07H: SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS (derivatives of aldonic or saccharic acids C07C, C07D; aldonic acids, saccharic acids C07C59/105, C07C59/285; cyanohydrins C07C255/16; glycals C07D; compounds of unknown constitution C07G; polysaccharides, derivatives thereof C08B; DNA or RNA concerning genetic engineering, vectors, e.g. plasmids, or their isolation, preparation or purification C12N15/00; sugar industry C13)
- C07B: GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR (preparation of carboxylic acid esters by telomerisation C07C67/47; telomerisation C08F)

## Abstract

The present invention provides compounds and methods of use thereof for treatment of certain disorders and conditions, for example brain injuries such as stroke or traumatic brain injuries.

## Claims

### Claim 1

A solid form of Compound A:
wherein said solid form has one or more peaks in its XRPD selected from those at about 8.0 and about 13.1 degrees 2-theta.

### Claim 2 (depends on 1)

The solid form according to claim 1, wherein said solid form is a crystalline solid substantially free of amorphous Compound A.

### Claim 3 (depends on 1)

The solid form according to claim 1, wherein said solid form is substantially free of impurities.

### Claim 4 (depends on 1)

The solid form according to claim 1, having two peaks in its XRPD selected from those at about 8.0 and about 13.1 degrees 2-theta.

### Claim 5 (depends on 1)

The solid form according to claim 1, having an XRPD substantially similar to that depicted in FIG. 1.

### Claim 6 (depends on 1)

A pharmaceutical composition comprising the solid form of claim 1 and a pharmaceutically acceptable carrier, excipient, or adjuvant.

### Claim 7

A solid form of Compound A:
wherein said solid form has one or more peaks in its XRPD selected from those at about 9.5, about 10.5, and about 13.8 degrees 2-theta.

### Claim 8 (depends on 7)

The solid form according to claim 7, having at least two peaks in its XRPD selected from those at about 9.5, about 10.5, and about 13.8 degrees 2-theta.

### Claim 9 (depends on 7)

The solid form according to claim 7, having an XRPD substantially similar to that depicted in FIG. 10.

### Claim 10 (depends on 7)

The solid form according to claim 7, wherein said solid form is a crystalline solid substantially free of amorphous Compound A.

### Claim 11 (depends on 7)

The solid form according to claim 7, wherein said solid form is substantially free of impurities.

### Claim 12 (depends on 7)

The solid form according to claim 7, having peaks in its XRPD at about 9.5, about 10.5, and about 13.8 degrees 2-theta.

### Claim 13 (depends on 7)

A pharmaceutical composition comprising the solid form of claim 7 and a pharmaceutically acceptable carrier, excipient, or adjuvant.