IP Library Granted Patent US 9,980,962
Granted Patent B2
US 9,980,962 · App. 15/647,688 · Granted May 29, 2018

Use of sulfonamide inhibitors of Bcl-2 to treat senescence-associated lung conditions such as pulmonary fibrosis and chronic obstructive pulmonary disease

Inventors: Remi-Martin Laberge (San Francisco, CA); Judith Campisi (Berkeley, CA); Marco Demaria (Groningen, NL); Nathaniel David (San Francisco, CA); Darren J. Baker (Rochester, MN); James L. Kirkland (Rochester, MN); Tamar Tchkonia (Rochester, MN); Jan M. A. van Deursen (Rochester, MN); Yi Zhu (Rochester, MN)
Assignees: UNITY BIOTECHNOLOGY, INC; BUCK INSTITUTE FOR RESEARCH ON AGING; MAYO FOUNDATION FOR MEDICAL EDUCATIOIN AND RESEARCH
A61K31/496A61K9/0073A61K31/404A61K31/428A61K31/4375A61K31/495A61K31/5377A61K45/06
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Quick Facts
Patent No.
US 9,980,962
App. No.
15/647,688
Granted
May 29, 2018
Kind
B2
Abstract

Methods are provided herein for selectively killing senescent cells and for treating senescence-associated diseases and disorders by administering a senolytic agent. Senescence-associated diseases and disorders treatable by the methods using the senolytic agents described herein include cardiovascular diseases and disorders associated with or caused by arteriosclerosis, such as atherosclerosis; idiopathic pulmonary fibrosis; chronic obstructive pulmonary disease; osteoarthritis; senescence-associated ophthalmic diseases and disorders; and senescence-associated dermatological diseases and disorders.

Claims (20)

1. A method of selectively eliminating senescent cells to relieve symptoms of a pulmonary disease or disorder that is not a cancer in a subject, the method comprising:

administering in or around a lung of a subject in need thereof a therapeutically effective course of therapy of a pharmaceutical composition that contains an aryl sulfonamide that selectively inhibits Bcl-xL;

wherein the pharmaceutical composition is formulated such that the aryl sulfonamide contacts senescent cells located in or around the lung that are causing symptoms of the pulmonary disease or disorder,

wherein the senescent cells are defined as non-cancerous cells that express p16,

wherein the therapeutically effective course of therapy includes:

(1) a treatment phase during which one or more doses of the pharmaceutical composition are administered to the subject so as to contact and selectively eliminate the senescent cells from the lung, followed by

(2) a therapeutic phase lasting at least two months, during which the pharmaceutical composition is not administered, and the symptoms of the pulmonary disease or disorder are relieved in the subject as a result of the selective elimination of the senescent cells by the administration of the one or more doses of the pharmaceutical composition during the treatment phase.

2. The method of claim 1 , wherein the aryl sulfonamide comprises the structure shown in Formula (II), or a pharmaceutically acceptable salt thereof:

wherein X 3 is Cl or F;

X 4 is azepan-1-yl, morpholin-4-yl, 1,4-oxazepan-4-yl, pyrrolidin-1-yl, N(CH 3 ) 2 , N(CH 3 )(CH(CH 3 ) 2 ), 7-azabicyclo[2.2.1]heptan-1-yl or 2-oxa-5-azabicyclo[2.2.1]hept-5-yl, and R 0 is

wherein X 5 is CH 2 , C(CH 3 ) 2 , or CH 2 CH 2 ; X 6 and X 7 are both hydrogen or are both methyl; and X 8 is F, Cl, Br or I; or

X 4 is azepan-1-yl, morpholin-4-yl, pyrrolidin-1-yl, N(CH 3 )(CH(CH 3 ) 2 ) or 7-azabicyclo[2.2.1]heptan-1-yl, and R 0 is

 or

X 4 is N(CH 3 ) 2 or morpholin-4-yl, and R 0 is

3. The method of claim 1 , wherein the aryl sulfonamide is ABT-737 or a pharmaceutically acceptable salt thereof.

4. The method of claim 1 , wherein the aryl sulfonamide is ABT-263 (Navitoclax) or a pharmaceutically acceptable salt thereof.

5. The method of claim 1 , wherein the aryl sulfonamide also inhibits Bcl-2.

6. The method of claim 1 , wherein the lung disease is chronic obstructive pulmonary disease.

7. The method of claim 1 , wherein the lung disease is lung damage caused by cigarette smoke.

8. The method of claim 1 , wherein the aryl sulfonamide is administered as an aerosol.

Assignments (6)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 10, 2018
From: ZHU, YI
To: MAYO FOUNDATION FOR MEDICAL EDUCATION AND RESEARCH
Reel/Frame 045492/0961 →
CONFIRMATORY LICENSE Recorded Sep 19, 2017
From: MAYO CLINIC ROCHESTER
To: NATIONAL INSTITUTES OF HEALTH (NIH), U.S. DEPT. OF HEALTH AND HUMAN SERVICES (DHHS), U.S. GOVERNMENT
Reel/Frame 043899/0152 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 1, 2017
From: LABERGE, REMI-MARTIN; CAMPISI, JUDITH; DAVALOS, ALBERT; DEMARIA, MARCO
To: BUCK INSTITUTE FOR RESEARCH ON AGING
Reel/Frame 043471/0115 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 1, 2017
From: DAVID, NATHANIEL; VASSEROT, ALAIN PHILIPPE
To: UNITY BIOTECHNOLOGY, INC.
Reel/Frame 043471/0312 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 1, 2017
From: BAKER, DARREN J.; CHILDS, BENNETT G.; KIRKLAND, JAMES L.; TCHKONIA, TAMAR; VAN DEURSEN, JAN M.A.; PALMER, ALLYSON K.
To: MAYO FOUNDATION FOR MEDICAL EDUCATION AND RESEARCH
Reel/Frame 043471/0433 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 1, 2017
From: ELISSEEFF, JENNIFER; KIM, CHAEKYU; JEON, OKHEE
To: THE JOHNS HOPKINS UNIVERSITY
Reel/Frame 043471/0625 →
Continuity (13)
Continuation 15114762
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Provisional Application 62057825 · Sep 30, 2014
Provisional Application 62057828 · Sep 30, 2014
Provisional Application 62061627 · Oct 8, 2014
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