HIV inhibitors

Patent metadata

Field	Value
Publication number	US-9309237-B2
Application number	US-201214241329-A
Country	US
Kind code	B2
Filing date	Sep 6, 2012
Priority date	Sep 6, 2011
Publication date	Apr 12, 2016
Grant date	Apr 12, 2016

Abstract

Chemical compounds that inhibit retroviruses are presented herein. More particularly, this disclosure provides small molecule compounds that inhibit infection with, or treat infection caused by, human immunodeficiency viruses.

First claim

What is claimed is:

1. A pharmaceutical composition comprising a compound represented by a formula:

wherein Ph 1 is phenyl optionally substituted with 1 or 2 substituents or cycloheptyl optionally substituted with 1 or 2 substituents, wherein each substituent is independently F, Cl, Br, R C , OR C , COR C , or R C —OH, wherein each R C is independently C 1-6 alkyl;
R t is a bond or C 1-3 alkyl;
Ar 1 is thiazolyl, pyridinyl, or phenyl optionally substituted with 1 or 2 substituents, wherein each substituent is independently F, Cl, Br, R C , OR C , COR C , or R C —OH, wherein each R C is independently C 1-6 alkyl; and
Cy 1 is piperidinyl, pyrrolidinyl, azepanyl, piperazinyl, or morpholino, optionally substituted with 1, 2, 3, or 4 substituents, wherein each substituent is independently F, Cl, Br, R C , OR C , COR C , or R C —OH, wherein each R C is independently C 1-6 alkyl;
and b is 0 or 1.

2. The pharmaceutical composition of claim 1 , wherein Cy 1 is —N(CH 2 CH 3 ) 2 or —CH 2 NHCH 3 .

3. The pharmaceutical composition of claim 1 , further represented by a formula:

wherein each R 1 , R 2 and R 3 is independently H, halogen, OH, or C 1 -C 6 alkyl optionally substituted with halogen or OH;
n is 1, 2, 3, 4 or 5;
o is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10;
p is 1, 2, 3, 4, 5, 6, 7 or 8;
a dashed line represents the presence or absence of a double bond; and
X 1 , X 2 and X 3 are each independently O, S, N, or C.

4. The composition of claim 3 , wherein if n is 1, then R 1 is not Br.

5. The composition of claim 1 , wherein the compound is:

6. A method for inhibiting infection with HIV or treating HIV infection comprising: administering to a patient in need thereof a composition comprising a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or ester thereof.

Assignees

• Debnath Asim Kumar
• Curreli Francesca
• Kwong Peter D
• Kwon Young Do
• New York Blood Ct Inc
• Us Health

Inventors

• Debnath Asim Kumar
• Curreli Francesca
• Kwong Peter D
• Kwon Young Do

Classifications

• C07D417/06

  linked by a carbon chain containing only aliphatic carbon atoms · CPC title

• A61K31/427

  not condensed and containing further heterocyclic rings · CPC title

• C07D211/42

  attached in position 3 or 5 · CPC title

• C07D213/81

  Amides; Imides · CPC title

• A61K31/167

  having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol · CPC title