IP Library Granted Patent US 11,667,615
Granted Patent B2
US 11,667,615 · App. 17/170,641 · Granted Jun 6, 2023

Certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamides as dipeptidyl peptidase 1 inhibitors

Inventors: Hans Roland Lönn (Cheshire, GB); Stephen Connolly (Cheshire, GB); Steven Swallow (Cheshire, GB); Staffan Po Karlsson (Mölndal, SE); Carl-Johan Aurell (Mölndal, SE); John Fritiof Pontén (Cheshire, GB); Kevin James Doyle (Essex, GB); Amanda Jane Van De Poël (Essex, GB); Graham Peter Jones (Essex, GB); David Wyn Watson (Essex, GB); Jaqueline Anne Macritchie (Essex, GB); Nicholas John Palmer (Cheshire, GB)
Assignee: AstraZeneca AB
C07D267/10A61K31/553A61K45/06C07D413/12C07D413/14C07D417/12
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Quick Facts
Patent No.
US 11,667,615
App. No.
17/170,641
Granted
Jun 6, 2023
Kind
B2
Abstract

The present disclosure relates to certain (2S)-N-[(1S)-1-cyano-2-phenylethyl]-1,4-oxazepane-2-carboxamide compounds (including pharmaceutically acceptable salts thereof), that inhibit dipeptidyl peptidase 1 (DPP1) activity, to their utility in treating and/or preventing clinical conditions including respiratory diseases, such as asthma and chronic obstructive pulmonary disease (COPD), to their use in therapy, to pharmaceutical compositions containing them and to processes for preparing such compounds.

Claims (45)

1. A method for treating alpha-1 antitrypsin deficiency in a patient in need thereof, comprising, administering to the patient, an effective amount of a compound of formula (I)

or a pharmaceutically acceptable salt thereof, wherein,

R 1 is

R 2 is selected from hydrogen, F, Cl, Br, OSO 2 C 1-3 alkyl, or C 1-3 alkyl;

R 3 is selected from hydrogen, F, Cl, Br, CN, CF 3 , SO 2 C 1-3 alkyl, CONH 2 or SO 2 NR 4 R 5 , wherein R 4 and R 5 together with the nitrogen atom to which they are attached form an azetidine, pyrrolidine or piperidine ring; or

R 1 is selected from

X is selected from O, S or CF 2 ;

Y is selected from O or S;

Q is selected from CH or N;

R 6 is selected from C 1-3 alkyl, wherein said C 1-3 alkyl is optionally substituted by 1, 2 or 3 F and optionally by one substituent selected from OH, OC 1-3 alkyl, N(C 1-3 alkyl) 2 , cyclopropyl, or tetrahydropyran; and

R 7 is selected from hydrogen, F, Cl or CH 3 .

2. The method of claim 1 , wherein R 1 is selected from

X is selected from O, S or CF 2 ;

Y is selected from O or S;

Q is selected from CH or N;

R 6 is selected from C 1-3 alkyl, wherein said C 1-3 alkyl is optionally substituted by 1, 2 or 3 F and optionally by one substituent selected from OH, OC 1-3 alkyl, N(C 1-3 alkyl) 2 , cyclopropyl, or tetrahydropyran; and

R 7 is selected from hydrogen, F, Cl or CH 3 .

3. The method of claim 1 , wherein,

R 1 is

X is selected from O, S or CF 2 ;

Y is selected from O or S;

R 6 is selected from C 1-3 alkyl, wherein said C 1-3 alkyl is optionally substituted by 1, 2 or 3 F and optionally by one substituent selected from OH, OC 1-3 alkyl, N(C 1-3 alkyl) 2 , cyclopropyl, or tetrahydropyran; and

R 7 is selected from hydrogen, F, Cl or CH 3 .

4. The method of claim 1 , wherein,

R 1 is

X is O;

R 6 is C 1-3 alkyl, wherein said C 1-3 alkyl is optionally substituted by 1, 2 or 3 F; and

R 7 is hydrogen.

5. The method of claim 1 , wherein,

R 1 is

6. The method of claim 4 , wherein,

R 1 is

X is O;

R 6 is C 1-3 alkyl; and

R 7 is hydrogen.

7. The method of claim 1 , wherein the compound of formula (I) is (2S)-N-{(1S)-1-cyano-2-[4-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-y-l)phenyl]ethyl}-1,4-oxazepane-2-carboxamide

or a pharmaceutically acceptable salt thereof.

8. The method of claim 7 , wherein the compound of formula (I) is (2S)-N-{(1S)-1-cyano-2-[4-(3-methyl-2-oxo-2,3-dihydro-1,3-benzoxazol-5-y-l)phenyl]ethyl}-1,4-oxazepane-2-carboxamide

9. The method of claim 1 , wherein the compound is present in a sterile solution, suspension or emulsion.

10. The method of claim 7 , wherein the compound is present in a sterile solution, suspension or emulsion.

11. The method of claim 10 , wherein administering comprises parenteral administration.

12. The method of claim 11 , wherein the parenteral administration is intravenous, subcutaneous, intramuscular, intravascular or infusion administration.

13. The method of claim 12 , wherein the parenteral administration is intravenous administration.

14. The method of claim 1 , wherein administering comprises oral administration.

15. The method of claim 7 , wherein administering comprises oral administration.

Assignments (7)
PATENT SECURITY AGREEMENT Recorded Oct 20, 2022
From: INSMED INCORPORATED
To: BIOPHARMA CREDIT PLC
Reel/Frame 061735/0875 →
SECOND LIEN PATENT SECURITY AGREEMENT Recorded Oct 19, 2022
From: INSMED INCORPORATED
To: ORBIMED ROYALTY & CREDIT OPPORTUNITIES IV, LP
Reel/Frame 061727/0039 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 24, 2021
From: ASTRAZENECA UK LIMITED
To: ASTRAZENECA AB
Reel/Frame 055386/0550 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 23, 2021
From: LÖNN, HANS ROLAND; PONTÉN, JOHN FRITIOF; AURELL, CARL-JOHAN; KARLSSON, STAFFAN PO
To: ASTRAZENECA AB
Reel/Frame 055378/0442 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 23, 2021
From: BIOFOCUS DPI LTD
To: ASTRAZENECA AB
Reel/Frame 055378/0424 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 23, 2021
From: DOYLE, KEVIN; VAN DE POËL, AMANDA; JONES, GRAHAM; WATSON, DAVID; MACRITCHIE, JAQUELINE; PALMER, NICHOLAS
To: BIOFOCUS DPI LTD
Reel/Frame 055378/0416 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 23, 2021
From: CONNOLLY, STEPHEN
To: ASTRAZENECA UK LIMITED
Reel/Frame 055378/0429 →