IP Library Granted Patent US 10,202,334
Granted Patent B2
US 10,202,334 · App. 15/838,012 · Granted Feb 12, 2019

Pendant amines and derivatives as inhibitors of leukotriene A4 hydrolase

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Quick Facts
Patent No.
US 10,202,334
App. No.
15/838,012
Granted
Feb 12, 2019
Kind
B2
Abstract

This present disclosure is directed to compounds of formula (I): where R 1a , R 1b , R 1c , R 1d , R 1e , R 3 , R 4a , R 4b , R 4c , R 4d , R 6 , R 7 , and R 8 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A 4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions including the compounds described herein and methods of preparing the compounds described herein are also provided.

Claims (24)

1. A compound selected from a formula in the Table below:

Compound

Compound Formula

Name

4-amino- N 1 -(4- phenoxy- phenyl) pentane- diamide

2-amino- N 1 -(2- chloro- ethyl)- N 5 -(4- phenoxy- phenyl) pentane- diamide

methyl N 5 -(4- (4-(1H- pyrrol-1- yl) phenoxy) phenyl) gluta- minate

(2R)-2- amino- N-(4- phenoxy- phenyl) pentane- diamide

methyl 3-{[(2R)- 2-amino- 4-[(4- phenoxy- phenyl) carba- moyl] butyl] carba- moyl} propan- oate

(2R)-2- amino-N- {4-[4- (1H- pyrrol-1- yl) phenoxy] phenyl)- N′-[2- (pyrrolidin- 1-yl)ethyl] pentano- diamide

(2S)-2- amino-N- [2- (pyridin- 2-yl)ethyl]- N′-{4-(4- (1H-pyrrol- 1-yl) phenoxy] phenyl} pentane- diamide

(2R)-2- amino-N- [2-(1H- imidazol- 5-yl) ethyl]-N′- {4-[4- (1H- pyrrol-1- yl) phenoxy) phenyl} pentane- diamide

ethyl 3- [(2R)-2- amino-4- [(4- phenoxy- phenyl) carbamoyl] butanamido] propanoate

methyl (2S)-2- amino-4- {[4- (phenyl- amino) phenyl] carbamoyl} butanoate.

2. A compound of the following formula

3. A compound of the following formula

4. A compound of the following formula

5. A compound of the following formula

6. A compound of the following formula

7. A compound of the following formula

8. A compound of the following formula

9. A compound of the following formula

10. A compound of the following formula

11. A compound of the following formula

Assignments (5)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 14, 2020
From: CELTAXSYS, INC.
To: CELLTAXIS, LLC
Reel/Frame 052665/0107 →
SECURITY INTEREST Recorded Oct 9, 2019
From: CELTAXSYS, INC.
To: DOMAIN PARTNERS VIII, L.P.; MASTERS, MICHAEL W.; INVUS PUBLIC EQUITIES, L.P.; LUMIRA CAPITAL II, L.P.; LUMIRA CAPITAL II (INTERNATIONAL), L.P.; GRA VENTURE FUND, LLC; GRA VENTURE FUND (T.E.), LLC; JWR, JR. FAMILY TRUST; ROGERS, JOE W., JR.; JOHNSON, WYATT THOMAS; 2007 STARR MOORE REVOCABLE TRUST
Reel/Frame 050666/0464 →
SECURITY INTEREST Recorded Sep 24, 2019
From: CELTAXSYS, INC.
To: DOMAIN PARTNERS VIII, L.P.; MASTERS, MICHAEL W.; MASTERS CAPITAL MANAGEMENT, LLC; MASTERS CAPITAL HEALTH VENTURES, LLC; INVUS PUBLIC EQUITIES, L.P.; LUMIRA CAPITAL II, L.P.; LUMIRA CAPITAL II (INTERNATIONAL), L.P.; GRA VENTURE FUND, LLC; GRA VENTURE FUND (T.E.), LLC; JWR, JR. FAMILY TRUST; ROGERS, JOE W., JR.; JOHNSON, WYATT THOMAS; 2007 STARR MOORE REVOCABLE TRUST
Reel/Frame 050469/0631 →
SECURITY INTEREST Recorded Nov 30, 2018
From: CELTAXSYS, INC.
To: DOMAIN PARTNERS VIII, L.P.; MASTERS, MICHAEL W.; MASTERS CAPITAL MANAGEMENT, LLC; MASTERS CAPITAL HEALTH VENTURES, LLC; INVUS PUBLIC EQUITIES, L.P.; LUMIRA CAPITAL II, L.P.; LUMIRA CAPITAL II (INTERNATIONAL), L.P.; GRA VENTURE FUND, LLC; GRA VENTURE FUND (T.E.), LLC; JWR, JR. FAMILY TRUST; ROGERS, JOE W., JR.; JOHNSON, WYATT THOMAS; 2007 STARR MOORE REVOCABLE TRUST
Reel/Frame 048172/0648 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 24, 2018
From: ROINESTAD, KURT; GUILFORD, WILLIAM; KIRKLAND, TOM; BHATT, LOPA; SPRINGMAN, ERIC
To: CELTAXSYS, INC.
Reel/Frame 045030/0661 →