# US 2019/0315775 A1 · Modified phenylphthalimide and pharmaceutical composition having same as active ingredient

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

- Number: US 2019/0315775 A1
- Document ID: US20190315775A1
- Status: Published application
- Kind: A1
- Application number: 16/343,130
- Filed: 2017-10-19
- Published: 2019-10-17
- Earliest claimed: 2016-10-21
- Assignees: Keio University; Idac Theranostics, Inc.
- Applicants: Keio University; Idac Theranostics, Inc.
- Inventors: Yutaka HATTORI; Maiko MATSUSHITA; Daiju ICHIKAWA; Shuji AIDA; Takeshi SUGAI; Taketo YAMADA; Hiroshi YANAGAWA; Yoko OGAWA; Noriko TABATA; Yuko YONEMURA
- Web page: https://patentgrep.com/patent/US20190315775A1

## CPC

- C07F 5/00: Compounds containing elements of Groups 3 or 13 of the Periodic Table
- A61K 47/60: the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol
- A61P 35/00: Antineoplastic agents
- C07D 209/48: with oxygen atoms in positions 1 and 3, e.g. phthalimide
- C07H 15/26: Acyclic or carbocyclic radicals, substituted by hetero rings
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)
- 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)

## Abstract

A phenylphthalimide derivative represented by the following general formula is provided as a phenylphthalimide derivative useful against various cancers including multiple myeloma, wherein R1 is a group containing PEG or a hydroxy C1-5 alkoxy group binding to position 4 or position 5, R2 is an amino group at position 6, and R3 and R4 are each independently a hydrogen atom, an alkyl group, an aryl group, an aralkyl group, or an aryloxy group.

## Claims

### Claim 1

A phenylphthalimide derivative represented by the following general formula:
wherein R1 is a group containing PEG or a hydroxy C1-5 alkoxy group binding to position 4 or position 5, R2 is an amino group at position 6, and R3 and R4 are each independently a hydrogen atom, an alkyl group, an aryl group, an aralkyl group, or an aryloxy group.

### Claim 2 (depends on 1)

The derivative according to claim 1, wherein R1 is a group containing PEG.

### Claim 3 (depends on 2)

The derivative according to claim 2, wherein R1 is a group in which PEG binds to a phthalimide ring via an ester bond.

### Claim 4 (depends on 1)

The derivative according to claim 1, wherein R1 is a hydroxy C1-5 alkoxy group.

### Claim 5 (depends on 1)

The derivative according to claim 1, wherein R1 binds to position 5.

### Claim 6 (depends on 1)

The derivative according to claim 1, wherein R3 and R4 are both isopropyl groups at position 2′ and position 6′, respectively.

### Claim 7 (depends on 1)

A pharmaceutical composition, comprising the derivative according to claim 1.

### Claim 8 (depends on 7)

The pharmaceutical composition according to claim 7, which is an anticancer agent.

### Claim 9 (depends on 8)

The pharmaceutical composition according to claim 8, wherein the anticancer agent is used for multiple myeloma.