# US 9,750,759 B2 · Antitumoral compounds

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

- Number: US 9,750,759 B2
- Document ID: US9750759B2
- Status: Granted
- Kind: B2
- Application number: 14/824,690
- Filed: 2015-08-12
- Published: 2015-12-03
- Granted: 2017-09-05
- Earliest claimed: 2015-08-12
- Assignees: Pharma Mar, S.A.
- Applicants: Pharma Mar, S.A.
- Inventors: Alberto Rodriquez Vicente; Maria Garranzo Garcia-Ibarrola; Carmen Murcia Perez; Francisco Sanchez Sancho; Maria del Carmen Cuevas Marchante; Cristina Mateo Urbano; Isabel Digon Juarez
- Web page: https://patentgrep.com/patent/US9750759B2

## CPC

- A61K 31/695: Silicon compounds
- A61K 31/351: not condensed with another ring
- A61K 31/366: having six-membered rings, e.g. delta-lactones
- A61P 35/00: Antineoplastic agents
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- C07D 309/10: Oxygen atoms
- C07D 309/30: Oxygen atoms, e.g. delta-lactones
- C07D 309/32: having two double bonds between ring members or between ring members and non-ring members
- C07F 7/1804: {Compounds having Si-O-C linkages (Si-O-acyl linkages C07F7/1896)}
- Y02P 20/55: Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
- 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)
- C07F: ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM (metal-containing porphyrins C07D487/22)
- Y02P: CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS

## Abstract

A compound of general formula (I) wherein A, Y, R1, R2, R3, R4, R5, and R6 take various meaning or use in the treatment of cancer.

## Claims

### Claim 1

A compound of general formula I
wherein Y is CHRay—CRby ═CRcy
each Ray, Rby, and Rcy is independently selected from hydrogen and unsubstituted C1-C12 alkyl;
each R1, R2, R3, R4, and R5 is independently selected from hydrogen and unsubstituted C1-C12 alkyl;
R6 is NR8R9;
A is
W is NR7;
R7 is hydrogen;
R8 is hydrogen;
each dotted line represents an optional additional bond, but when a triple bond exists between the C atoms to which R1 and R2 are attached, R1 and R2 are absent, and when a triple bond exists between the C atoms to which R3 and R4 are attached, R3 and R4 are absent;
R9 is selected from substituted or unsubstituted C2-C12 alkenyl and substituted or unsubstituted C4-C12 alkenynyl wherein the optional substituents are selected from halogen atoms and OR′, wherein R′ is hydrogen, silyl-ether protecting group or CONR″R″ wherein each R″ is independently selected from hydrogen and C1-C6 alkyl;
each R16, R17 and R18 are independently selected from hydrogen and ORa;
R19 is hydrogen; and
Ra is unsubstituted C1-C12 alkyl; or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof.

### Claim 2 (depends on 1)

The compound according to claim 1, wherein R16 is selected from hydrogen and ORa , wherein Ra is unsubstituted C1-C6 alkyl.

### Claim 3 (depends on 2)

The compound according to claim 2, wherein R16 is selected from hydrogen and methoxy.

### Claim 4 (depends on 1)

The compound according to claim 1, wherein one additional bond is present between the C atoms to which R16 and R17 are attached.

### Claim 5 (depends on 1)

The compound according to claim 1, wherein R17 and R18 are hydrogen.

### Claim 6 (depends on 1)

The compound according to claim 1, wherein R1, R2, R3 and R4 are independently selected from hydrogen and unsubstituted C1-C6 alkyl.

### Claim 7 (depends on 6)

The compound according to claim 6, wherein R1, R2, R3 and R4 are hydrogen.

### Claim 8 (depends on 1)

The compound according to claim 1, wherein Ray, Rby and Rcy are independently selected from hydrogen and unsubstituted C1-C6 alkyl.

### Claim 9 (depends on 8)

The compound according to claim 8, wherein Ray, Rby and Rcy are independently selected from hydrogen and methyl.

### Claim 10 (depends on 1)

The compound according to claim 1, wherein R5 is selected from hydrogen and unsubstituted C1-C6 alkyl.

### Claim 11 (depends on 10)

The compound according to claim 10, wherein R5 is selected from methyl, isopropyl and tert-butyl.

### Claim 12 (depends on 1)

The compound according to claim 1, wherein one additional bond is present between the C atoms to which R1 and R2 are attached and one or two additional bonds are present between the C atoms to which R3 and R4 are attached.

### Claim 13 (depends on 1)

The compound according to claim 1, having the following formula:
or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof.

### Claim 14 (depends on 1)

A pharmaceutical composition comprising a compound according to claim 1, or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, and a pharmaceutically acceptable diluent or carrier.