Method of treatment

Patent metadata

Field	Value
Publication number	US-2019300479-A1
Application number	US-201716317269-A
Country	US
Kind code	A1
Filing date	Jul 13, 2017
Priority date	Jul 21, 2016
Publication date	Oct 3, 2019
Grant date	—

Abstract

Lactams for use in the treatment of respiratory tract infections, including chronic lung infections in patients having cystic fibrosis.

First claim

1 . A method of treatment of a respiratory tract infection in a subject comprising:
administering to the subject an effective amount of a lactam of Formula I or Formula II

wherein Ar is an unsubstituted or substituted phenyl and R 1 is H or C 1-4 alkyl.

2 . The method of claim 1 , wherein the respiratory tract infection is a bacterial lung infection.

3 . The method of claim 1 , wherein the subject has cystic fibrosis.

4 . The method of claim 1 , wherein Ar has a substituent at the 4-position.

5 . The method of claim 1 , wherein the lactam is a lactam of Formula Ia or Formula IIa:

wherein
R 1 is H; and
R 2 is H, halogen, or C 1-4 alkyl.

6 . The method of claim 5 , wherein R 2 is Cl, F or Me.

7 . The method of claim 1 , wherein the lactam is at least one of:
4-(4-chlorophenyl)-5-methylene-pyrrol-2-one; 5-methylene-4-(p-tolyl)pyrrol-2-one; 4-(4-fluorophenyl)-5-methylene-pyrrol-2-one; 4-phenyl-5-hydroxy-5-methyl-1H-pyrrol-2-one; 4-(4-fluorophenyl)-5-hydroxy-5-methyl-1H-pyrrol-2-one; 4-(4-bromophenyl)-5-hydroxy-5-methyl-1H-pyrrol-2-one; 4-phenyl-5-methylene-pyrrol-2-one; 4-(4-bromophenyl)-5-methylene-pyrrol-2-one; 4-(2-fluorophenyl)-5-methylene-pyrrol-2-one; 4-(4-chlorophenyl)-5-hydroxy-5-methyl-1H-pyrrol-2-one; 4-(2-chlorophenyl)-5-hydroxy-5-methyl-1H-pyrrol-2-one; 4-(2-chlorophenyl)-5-methylene-pyrrol-2-one; 4-(3-chlorophenyl)-5-methylene-pyrrol-2-one; 4-(3-chlorophenyl)-5-hydroxy-5-methyl-1H-pyrrol-2-one; 4-(4-chlorophenyl)-1-methyl-5-methylene-pyrrol-2-one; or 4-(4-hydroxy-3-methoxy-phenyl)-5-methylene-pyrrol-2-one.

8 . The method of claim 1 , wherein the lactam is 4-(4-chlorophenyl)-5-methylene-pyrrol-2-one.

9 . A pharmaceutical composition comprising,
a lactam of Formula I or Formula II

wherein Ar is an unsubstituted or substituted phenyl and R 1 is H or C 1-4 alkyl
wherein the pharmaceutical composition is formulated for parenteral administration.

10 . A pharmaceutical composition,
a lactam of Formula I or Formula II

wherein Ar is an unsubstituted or substituted phenyl and R 1 is H or C 1-4 alkyl
wherein the pharmaceutical composition is formulated for administration by insufflation and/or inhalation.

11 . The lactam of claim 4 , wherein the substituent at the 4-position is chloro or methyl.

Assignees

• Conopco Inc Dba Unilever

Inventors

• Parry Neil James
• Pantalone Paolo
• Williams Paul

Classifications

• A61P31/00

  Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics · CPC title

• A61P31/04

  Antibacterial agents · CPC title

• A61P11/00

  Drugs for disorders of the respiratory system · CPC title

• A61K9/0073

  Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy; (nasal sprays A61K9/0043; inhalation of vapours of volatile or heated drugs, e.g. essential oils or nicotine, A61K9/007; devices A61M) · CPC title

• A61K31/4015

  having oxo groups directly attached to the heterocyclic ring, e.g. piracetam, ethosuximide · CPC title