# US 8,772,281 B2 · Remedy for diabetes

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- Number: US 8,772,281 B2
- Document ID: US8772281B2
- Status: Granted
- Kind: B2
- Application number: 13/709,798
- Filed: 2012-12-10
- Published: 2013-05-23
- Granted: 2014-07-08
- Earliest claimed: 2007-04-11
- Assignees: Ajinomoto Co., Inc.
- Applicants: Ajinomoto Co., Inc.
- Inventors: Naoyuki Fukuchi; Satoru Okamoto; Wataru Miyanaga; Sen Takeshita; Masaru Takayanagi; Yumiko Fukuda; Takao Ikenoue; Naoyuki Yamada; Naoko Arashida
- Web page: https://patentgrep.com/patent/US8772281B2

## CPC

- C07D 487/04: Ortho-condensed systems
- A61K 31/55: having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K 31/551: having two nitrogen atoms, e.g. dilazep
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 13/12: of the kidneys
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 27/02: Ophthalmic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 519/00: Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
- C12Q 1/485: {involving kinase}
- G01N 33/5035: {on sub-cellular localization}
- G01N 33/573: for enzymes or isoenzymes
- G01N 33/6845: {Methods of identifying protein-protein interactions in protein mixtures}
- G01N 33/6872: {Intracellular protein regulatory factors and their receptors, e.g. including ion channels}
- G01N 2333/4719: G-proteins
- G01N 2333/91215: with a definite EC number (2.7.1.-)
- G01N 2500/04: Screening involving studying the effect of compounds C directly on molecule A (e.g. C are potential ligands for a receptor A, or potential substrates for an enzyme A)
- G01N 2800/042: Disorders of carbohydrate metabolism, e.g. diabetes, glucose metabolism
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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
- C12Q: MEASURING OR TESTING PROCESSES INVOLVING ENZYMES, NUCLEIC ACIDS OR MICROORGANISMS (immunoassay G01N33/53); COMPOSITIONS OR TEST PAPERS THEREFOR; PROCESSES OF PREPARING SUCH COMPOSITIONS; CONDITION-RESPONSIVE CONTROL IN MICROBIOLOGICAL OR ENZYMOLOGICAL PROCESSES
- G01N: INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES (measuring or testing apparatus or processes other than immunoassay, involving enzymes or microorganisms C12M, C12Q)

## Abstract

A method of screening a compound having a hypoglycemic effect (hereinafter referred to as “hypoglycemic compound”), a remedy for diabetes which contains a compound having a novel function mechanism, etc. More specifically speaking, a method of screening a hypoglycemic compound capable of binding to the β subunit of a trimeric GTP-binding protein, a remedy for diabetes comprising a hypoglycemic compound, which is characterized by being capable of binding to the β subunit of a trimeric GTP-binding protein, as the active ingredient, etc.

## Claims

### Claim 1

A compound represented by general formula (I) or a pharmaceutically acceptable salt thereof:
wherein
in the general formula (I), A and B may be the same or different and independently represent an optionally substituted aromatic ring, an optionally substituted heterocyclic ring, or an optionally substituted aliphatic ring;
R1 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, or a lower alkoxy group, the groups being optionally substituted by 1 to 3 substituents;
—X— and —Y— may be the same or different and independently represent a hydrogen atom, —O—, —NR2—, —S—, —SO—, —SO2—, —CH2—, —CR3R4—, —COO—, —CONR2—, or —CO—, in which R2 represents a hydrogen atom, an optionally substituted lower alkyl group, an optionally substituted acyl group, an optionally substituted alkoxycarbonyl group, an optionally substituted carbamoyl group, or an optionally substituted sulfonyl group, and R3 and R4 may be the same or different and independently represent a hydrogen atom, a halogen atom, a hydroxyl group, an alkyl group, a mercapto group, an alkoxy group, an alkylthio group, an alkylsulfonyl group, an acyl group, an acyloxy group, an amino group, an alkylamino group, a carboxyl group, an alkoxycarbonyl group, a carbamoyl group, a nitro group, a cyano group, or a trifluoromethyl group;
—W— represents an optionally substituted alkyl chain having 1 to 20 carbon atoms, and 1 to 10 carbon atoms in the alkyl chain may be replaced by —O—, —NR5—, —S—, —SO—, —SO2—, or —CO—, in which R5 represents a hydrogen atom, an optionally substituted lower alkyl group, an optionally substituted acyl group, an optionally substituted alkoxycarbonyl group, an optionally substituted carbamoyl group, or an optionally substituted sulfonyl group;
Q represents a hydrogen atom, biotin, a fluorophore, a chromophore, a chemiluminescent functional group, an enzyme, a solid phase, a diazo group, or an azido group;
one or more atoms in the formula may be (a) radioisotope(s);
with the proviso that:
i) in the optionally substituted groups, each substituent is selected from the group consisting of halogen atoms, a hydroxyl group, alkyl groups, mercapto groups, alkoxy groups, alkylthio groups, alkylsulfonyl groups, acyl groups, acyloxy groups, amino groups, alkylamino groups, a carboxyl group, alkoxycarbonyl groups, carbamoyl groups, a nitro group, a cyano group, a trifluoromethyl group, aryl groups, heteroaryl groups, diazo groups, and azido groups, and the substituent may be labeled with biotin, a fluorophore, a chromophore, a chemiluminescent moiety, or an enzyme;
ii) when —X— is a hydrogen atom, —W—, —Y—, and Q do not exist;
iii) when —Y— is a hydrogen atom, Q does not exist; and
iv) the compound of the general formula (I) satisfies at least one of the following conditions a) to f):
a) —X— and —Y— are other than a hydrogen atom, and Q is biotin, a fluorophore, a chromophore, a chemiluminescent functional group, or an enzyme;
b) —X— and —Y— are other than a hydrogen atom, and Q is a diazo group or an azido group;
c) —X— and —Y— are other than a hydrogen atom, and Q is a solid phase;
d) labeled with at least one radioisotope atom;
e) substituted with at least one substituent which is labeled with biotin, a fluorophore, a chromophore, a chemiluminescent moiety, or an enzyme; or
f) substituted with at least one diazo group or azido group as a substituent.

### Claim 2 (depends on 1)

A compound or a pharmaceutically acceptable salt thereof according to claim 1, wherein —X— and —Y— are other than a hydrogen atom, and Q is biotin, a fluorophore, a chromophore, a chemiluminescent functional group, or an enzyme.

### Claim 3 (depends on 2)

A compound or a pharmaceutically acceptable salt thereof according to claim 2, wherein each substituent in the optionally substituted groups is not labeled with biotin, a fluorophore, a chromophore, a chemiluminescent moiety, or an enzyme.

### Claim 4 (depends on 1)

A compound or a pharmaceutically acceptable salt thereof according to claim 1, wherein —X— and —Y— are other than a hydrogen atom, and Q is a diazo group or an azido group.

### Claim 5 (depends on 4)

A compound or a pharmaceutically acceptable salt thereof according to claim 4, wherein each substituent in the optionally substituted groups is not labeled with biotin, a fluorophore, a chromophore, a chemiluminescent moiety, or an enzyme.

### Claim 6 (depends on 1)

A compound or a pharmaceutically acceptable salt thereof according to claim 1, wherein —X— and —Y— are other than a hydrogen atom, and Q is a solid phase.

### Claim 7 (depends on 1)

A compound or a pharmaceutically acceptable salt thereof according to claim 1, wherein at least one atom in the general formula (I) is a radioisotope.

### Claim 8 (depends on 7)

A compound or a pharmaceutically acceptable salt thereof according to claim 7, wherein X is a hydrogen atom.

### Claim 9 (depends on 1)

A compound or a pharmaceutically acceptable salt thereof according to claim 1, wherein the compound has at least one substituent which is labeled with biotin, a fluorophore, a chromophore, a chemiluminescent moiety, or an enzyme.

### Claim 10 (depends on 1)

A compound or a pharmaceutically acceptable salt thereof according to claim 1, wherein the compound has at least one diazo group or azido group as a substituent.