# US 2019/0314352 A1 · Administration of dipeptidyl peptidase inhibitors

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- Number: US 2019/0314352 A1
- Document ID: US20190314352A1
- Status: Published application
- Kind: A1
- Application number: 16/277,537
- Filed: 2019-02-15
- Published: 2019-10-17
- Earliest claimed: 2005-09-14
- Assignees: Takeda Pharmaceutical Company Limited
- Applicants: Takeda Pharmaceutical Company Limited
- Inventors: Ronald J. Christopher; Paul Covington
- Web page: https://patentgrep.com/patent/US20190314352A1

## CPC

- A61K 31/4439: containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole (nicotine A61K31/465)
- A61K 31/131: acyclic
- A61K 31/155: Amidines ([IMAGE cpc-sch-A61K-1029.gif]), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
- A61K 31/44: Non condensed pyridines; Hydrogenated derivatives thereof
- A61K 31/513: having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 1/02: Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
- A61P 1/04: for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
- A61P 1/14: Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
- A61P 3/00: Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00)
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/06: Antihyperlipidemics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 9/00: Drugs for disorders of the cardiovascular system
- A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- A61P 9/12: Antihypertensives
- A61P 11/08: Bronchodilators
- A61P 13/12: of the kidneys
- A61P 25/00: Drugs for disorders of the nervous system
- A61P 25/02: for peripheral neuropathies
- A61P 25/04: Centrally acting analgesics, e.g. opioids
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 37/08: Antiallergic agents (antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14)
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07C 257/06: having carbon atoms of imino-carboxyl groups bound to hydrogen atoms, to acyclic carbon atoms, or to carbon atoms of rings other than six-membered aromatic rings
- C07C 317/40: Y being a hydrogen or a carbon atom
- C07D 209/26: with an acyl radical attached to the ring nitrogen atom
- C07K 16/2896: {against molecules with a "CD"-designation, not provided for elsewhere}
- C07K 16/40: against enzymes
- A61K 2039/505: {comprising antibodies}
- C07C 2602/08: the other ring being five-membered, e.g. indane
- C07K 2317/76: Antagonist effect on antigen, e.g. neutralization or inhibition of binding
- 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
- C07C: ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07D: HETEROCYCLIC COMPOUNDS (macromolecular compounds C08)
- 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)

## Abstract

Pharmaceutical compositions comprising 2-[[6-[(3R)-3-amino-1-piperidinyl]-3,4-dihydro-3-methyl-2,4-dioxo-1 (2H)-pyrimidinyl]methyl]-benzonitrile and pharmaceutically acceptable salts thereof are provided as well as kits and articles of manufacture comprising the pharmaceutical compositions as well as methods of using the pharmaceutical compositions.

## Claims

### Claim at position 1

1-96. (canceled)

### Claim 97

A method of treating type II diabetes mellitus in a patient in need thereof, the method comprising administering to the patient between 5 mg and 250 mg of Compound I, wherein Compound I has the formula
or a pharmaceutically acceptable salt thereof, in combination with between 125 mg and 2550 mg of metformin or a pharmaceutically acceptable salt thereof.

### Claim 98 (depends on 97)

The method of claim 97, wherein between 10 mg and 150 mg of Compound I is administered.

### Claim 99 (depends on 97)

The method of claim 97, wherein between 10 mg and 100 mg of Compound I is administered.

### Claim 100 (depends on 97)

The method of claim 97, wherein 12.5 mg of Compound I is administered.

### Claim 101 (depends on 97)

The method of claim 97, wherein 20 mg of Compound I is administered.

### Claim 102 (depends on 97)

The method of claim 97, wherein 25 mg of Compound I is administered.

### Claim 103 (depends on 97)

The method of claim 97, wherein 50 mg of Compound I is administered.

### Claim 104

A method of treating type II diabetes mellitus in a patient in need thereof, the method comprising administering to the patient between 5 mg and 250 mg of Compound I, wherein Compound I has the formula
or a pharmaceutically acceptable salt thereof, in combination with between 7.5 mg and 60 mg of pioglitazone or a pharmaceutically acceptable salt thereof.

### Claim 105 (depends on 104)

The method of claim 104, wherein between 10 mg and 150 mg of Compound I is administered.

### Claim 106 (depends on 104)

The method of claim 104, wherein between 10 mg and 100 mg of Compound I is administered.

### Claim 107 (depends on 104)

The method of claim 104, wherein 12.5 mg of Compound I is administered.

### Claim 108 (depends on 104)

The method of claim 104, wherein 20 mg of Compound I is administered.

### Claim 109 (depends on 104)

The method of claim 104, wherein 25 mg of Compound I is administered.

### Claim 110 (depends on 104)

The method of claim 104, wherein 50 mg of Compound I is administered.

### Claim 111 (depends on 104)

The method of claim 104, comprising pioglitazone hydrochloride.

### Claim 112

A method of treating type II diabetes mellitus in a patient in need thereof, the method comprising administering to the patient between 5 mg and 250 mg of Compound I, wherein Compound I has the formula
or a pharmaceutically acceptable salt thereof, in combination with between 125 mg and 2550 mg of metformin or pharmaceutically acceptable salt thereof, and between 7.5 mg and 60 mg of pioglitazone or a pharmaceutically acceptable salt thereof.

### Claim 113 (depends on 112)

The method of claim 112, wherein between 10 mg and 150 mg of Compound I is administered.

### Claim 114 (depends on 112)

The method of claim 112, wherein between 10 mg and 100 mg of Compound I is administered.

### Claim 115 (depends on 112)

The method of claim 112, wherein 12.5 mg of Compound I is administered.

### Claim 116 (depends on 112)

The method of claim 112, wherein 20 mg of Compound I is administered.

### Claim 117 (depends on 112)

The method of claim 112, wherein 25 mg of Compound I is administered.

### Claim 118 (depends on 112)

The method of claim 112, wherein 50 mg of Compound I is administered.