# US 2019/0167702 A1 · Use of derivatives containing c-o-p bonds in patients with kidney failure

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- Number: US 2019/0167702 A1
- Document ID: US20190167702A1
- Status: Published application
- Kind: A1
- Application number: 16/209,150
- Filed: 2018-12-04
- Published: 2019-06-06
- Earliest claimed: 2013-03-15
- Assignees: Laboratoris Sanifit, S.L.
- Applicants: Laboratoris Sanifit, S.L.
- Inventors: Joan PERELLO BESTARD; Carolina SALCEDO ROCA; Miguel David FERRER REYNES; Bernat ISERN AMENGUAL; Pieter H. JOUBERT
- Web page: https://patentgrep.com/patent/US20190167702A1

## CPC

- A61K 31/6615: Compounds having two or more esterified phosphorus acid groups, e.g. inositol triphosphate, phytic acid
- A61K 9/0019: {Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner (non-active ingredients are additionally classified in A61K47/00)}
- A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration}
- A61K 31/135: having aromatic rings {, e.g. ketamine, nortriptyline (methadone A61K31/137)}
- A61K 31/59: Compounds containing 9, 10- seco- cyclopenta[a]hydrophenanthrene ring systems
- A61K 31/663: Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
- A61K 31/785: Polymers containing nitrogen
- A61K 33/04: Sulfur, selenium or tellurium; Compounds thereof
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- 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)

## Abstract

Use of a derivative containing C—O—P bonds in a controlled release form to treat patients with kidney failure. Moreover, it comprises the use of said derivatives together with other active substances, which particularly may be selected from a list comprising a calcimimetic, vitamin, phosphate binder, thiosulfate, bisphosphonate, pyrophosphate, citrate, diuretic, antihypertensive and anticholesteraemic agent.

## Claims

### Claim 1

A method for the treatment and/or prevention of a kidney failure-related disease in a subject with kidney failure comprising administering to a subject in need an effective amount of a medicament which comprises at least one compound of formula I, or a pharmaceutical acceptable salt thereof:
where:
each R1 to R12 independently represents H, —X, —OX, —NHX, —SX, —OSO3HX, —OSO3X2 or a compound of formula II:
where each X independently represents H, C1-30alkyl, C2-30alkenyl, C2-30alkynyl or Cy1, where C1-30alkyl, C2-30alkenyl and C2-30alkynyl are independently optionally substituted by one or more R14 and where Cy1 is optionally substituted by one or more R15;
Cy1 represents a carbocyclic or heterocyclic three- to 10-membered ring, which may be saturated, partially unsaturated or aromatic, where said heterocycle has between one and four heteroatoms selected from amongst O, S and N, where said ring can be bound to the rest of the molecule via any available C atom and where Cy1 optionally fused to between one and four five- or six-membered rings, each saturated, partially unsaturated or aromatic, carbocyclic or heterocyclic, and where said fused heterocycle may contain one or two heteroatoms selected from amongst O, N and S;
each R13 independently represents H, C1-30alkyl, —NH2, —NHC1-30alkyl or —N(C1-30alkyl)2, where each C1-30alkyl is independently optionally substituted with one or more halogen, —OH, —CN and —NO2 groups; and
each R14 and R15 independently represents —OH, C1-30alkoxy, C1-30alkylthionyl, C1-30acyloxy, phosphate, halogen, trihaloC1-30alkyl, nitrile or azide,
with the condition that at least one of R1 to R12 independently represents a compound of formula II,
characterised in that said medicament is administered in a prolonged release form.

### Claim 2 (depends on 1)

The method according to claim 1, where:
each X independently represents H, C1-30alkyl or Cy1, where C1-30alkyl is optionally substituted by one or more R14 and where Cy1 is optionally substituted by one or more R15; and
each R14 and R15 independently represents —OH, C1-30alkoxy, C1-30alkylthionyl, C1-30acyloxy, phosphate, halogen, trihaloC1-30alkyl, nitrile or azide.

### Claim 3 (depends on 1)

The method according to claim 1, where:
each X represents H, C1-30alkyl or Cy1.

### Claim 4 (depends on 1)

The method according to claim 1, where:
each X represents H.

### Claim 5 (depends on 1)

The method according to claim 1, where:
At least one of radicals R1, R3, R5, R7, R9 and R11 independently represents a compound of formula II:
where each R13 independently represents H, C1-30alkyl, —NH2, —NHC1-30alkyl or —N(C1-30alkyl)2, where each C1-30alkyl is independently optionally substituted by one or more halogen, —OH, —CN and —NO2 groups; and
R2, R4, R6, R8, R10 and R12 independently represent H.

### Claim 6 (depends on 1)

The method according to claim 1, where:
R1, R3, R5, R7, R9 and R11 independently represent a compound of formula II:
each R13 independently represents H or C1-30alkyl, where each C1-30alkyl is independently optionally substituted by one or more halogen, —OH, —CN and —NO2 groups; and
R2, R4, R6, R8, R10 and R12 independently represent H.

### Claim 7 (depends on 1)

The method according to claim 1, where:
R1, R3, R5, R7, R9 and R11 independently represent a compound of formula II:
each R13 independently represents H or C1-30alkyl; and
R2, R4, R6, R8, R10 and R12 independently represent H.

### Claim 8 (depends on 1)

The method according to claim 1, where:
R1, R3, R5, R7, R9 and R11 independently represent a compound of formula II:
each R13 independently represents H; and
R2, R4, R6, R8, R10 and R12 independently represent H.

### Claim 9 (depends on 1, 2, 3, 4, 5, 6, 7, 8)

A method for the treatment and/or prevention of a kidney failure-related disease in a subject with kidney failure comprising administering to a subject in need an effective amount of a medicament which comprises a composition comprising at least one compound of general formula I as described in claims 1 to 8 and another active substance characterised in that said medicament is administered in a prolonged release form.

### Claim 10 (depends on 9)

The method according to claim 9, where the active substance is selected from a list comprising a calcimimetic, vitamin, phosphorus chelator, thiosulfate, bisphosphonate, pyrophosphate, citrate, diuretic, antihypertensive and anticholesteraemic agent.

### Claim 11 (depends on 1, 2, 3, 4, 5, 6, 7, 8)

A method for the treatment and/or prevention of a kidney failure-related disease in a subject with kidney failure comprising administering to a subject in need an effective amount of a medicament which comprises a combined preparation composing at least one compound of general formula I as described in claims 1 to 8 and a compound selected from a list comprising a calcimimetic, vitamin B, vitamin D or vitamin K, phosphorus chelator, thiosulfate, bisphosphonate, pyrophosphate, citrate, diuretic, antihypertensive and anticholesteraemic agent separately, simultaneously or sequentially.

### Claim 12 (depends on 1, 9, 11)

The method according to any of claims 1, 9 or 11, where the kidney failure-related diseases are calcium disorder-related diseases.

### Claim 13 (depends on 1, 9, 11)

The method according to any of claims 1, 9 or 11, where the calcium disorder-related diseases are selected from the list comprising renal lithiasis, cardiovascular calcification, cardiovascular disease, osteoporosis, bone cancer, podagra, calcific tendinitis, calcinosis cutis, rheumatoid arthritis, bone mineral disease, osteomalacia, adynamic bone, calciphylaxis and cardiovascular diseases.

### Claim 14 (depends on 1, 9, 11)

The method according to any of claims 1, 9 or 11, where the medicinal product is found in a form suitable for parenteral, topical or enteral administration.