# US 11,299,587 B2 · Starting material, for bulk drug or additives for drug, and bulk drug or drug using same

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- Number: US 11,299,587 B2
- Document ID: US11299587B2
- Status: Granted
- Kind: B2
- Application number: 16/957,203
- Filed: 2018-12-21
- Published: 2021-11-25
- Granted: 2022-04-12
- Earliest claimed: 2017-12-27
- Assignees: Sanyo Chemical Industries, Ltd.
- Applicants: Sanyo Chemical Industries, Ltd.
- Inventors: Shihei Motofuji; Kenichiro Nakai; Kyosuke Michigami; Itsuka Matsumoto
- Web page: https://patentgrep.com/patent/US11299587B2

## CPC

- C08G 65/33337: {cyclic}
- A61K 47/10: Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
- C08G 65/2609: {containing aliphatic hydroxyl groups}
- C08G 65/332: containing carboxyl groups, or halides, or esters thereof
- C08G 65/3322: {acyclic}
- C08G 65/3328: {heterocyclic}
- C08G 65/333: containing nitrogen
- C08L 71/02: Polyalkylene oxides
- C08G: MACROMOLECULAR COMPOUNDS OBTAINED OTHERWISE THAN BY REACTIONS ONLY INVOLVING UNSATURATED CARBON-TO-CARBON BONDS
- 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)
- C08L: COMPOSITIONS OF MACROMOLECULAR COMPOUNDS (compositions based on polymerisable monomers C08F, C08G; artificial filaments or fibres D01F; textile treating compositions D06)

## Abstract

The present invention provides a raw material for bulk drugs and a pharmaceutical additive which provide excellent formulation stability and excellent over-time stability of drug efficacy when used to modify a bulk drug, a polypeptide, a bioactive protein, an enzyme, and the like. The present invention relates to a raw material for bulk drugs or a pharmaceutical additive, containing: a polyether composition (A) represented by formula (1), wherein the polyether composition (A) has a unimodal molecular weight distribution, the polyether composition (A) has a ratio (Mw/Mn) of the weight average molecular weight (Mw) to the number average molecular weight (Mn) of 1.20 or less, and the polyether composition (A) contains a compound in which m is 1 in formula (1) in an amount of 90 wt % or more based on the weight of the polyether composition (A), in formula (1), OR1, R2O, R3O, and R4O are each independently a C2-C8 oxyalkylene group; when each of these moieties exists in the plural number, each OR1, each R2O, each R3O, and each R4O may be the same as or different from each other; these moieties may be bonded randomly or in block; a, b, c, and d are each independently an integer of 50 to 1200; X1 to X4 are each independently a hydrogen atom, a substituent represented by formula (2), or a substituent represented by formula (3); and m is an integer of 1 to 10.

## Claims

### Claim 1

A raw material for bulk drugs or a pharmaceutical additive, comprising:
a polyether composition (A) represented by formula (1),
wherein the polyether composition (A) has a unimodal molecular weight distribution,
the polyether composition (A) has a ratio (Mw/Mn) of the weight average molecular weight (Mw) to the number average molecular weight (Mn) of 1.20 or less, and
the polyether composition (A) contains a compound in which m is 1 in formula (1) in an amount of 90 wt % or more based on the weight of the polyether composition (A),
in formula (1), OR1, R2O, R3O, and R4O are each independently a C2-C8 oxyalkylene group; when each of these moieties exists in the plural number, each OR′, each R2O, each R3O, and each R4O may be the same as or different from each other; these moieties may be bonded randomly or in block; a, b, c, and d are each independently an integer of 50 to 1200; X1 to X4 are each independently a hydrogen atom, a substituent represented by formula (2), or a substituent represented by formula (3); and m is an integer of 1 to 10,
in formulas (2) and (3), R6 is a C1-C10 alkylene group; in formula (2), R7 is a hydrogen atom or a C1-C15 monovalent hydrocarbon group in which a hydrogen atom may be replaced by a C1-C10 alkoxy group; and when a substituent represented by formula (2) or (3) exists in the plural number in formula (1), each R6 and each R7 in these substituents may be the same as or different from each other.

### Claim 2 (depends on 1)

The raw material for bulk drugs or the pharmaceutical additive according to claim 1
wherein each of OR1, R2O, R3O, and R4O in formula (1) is an oxyethylene group.

### Claim 3 (depends on 1)

The raw material for bulk drugs or the pharmaceutical additive according to claim 1,
wherein the amount of the polyether composition (A) is 0.1 to 99.5 wt % based on the weight of the raw material for bulk drugs or the pharmaceutical additive.

### Claim 4 (depends on 1)

A bulk drug or a pharmaceutical product, comprising:
the raw material for bulk drugs or the pharmaceutical additive according to claim 1.

### Claim 5 (depends on 2)

The raw material for bulk drugs or the pharmaceutical additive according to claim 2,
wherein the amount of the polyether composition (A) is 0.1 to 99.5 wt % based on the weight of the raw material for bulk drugs or the pharmaceutical additive.

### Claim 6 (depends on 2)

A bulk drug or a pharmaceutical product, comprising:
the raw material for bulk drugs or the pharmaceutical additive according to claim 2.