US2019300490A1PendingUtilityA1
Saturated-ring-fused dihydropyrimidinone or dihydrotriazinone compounds and pharmaceutical use thereof
Est. expiryFeb 28, 2038(~11.6 yrs left)· nominal 20-yr term from priority
C07D 239/80C07D 491/052C07D 498/04C07D 239/70C07D 487/04C07D 491/048C07D 239/82A61P 9/12A61P 37/00A61K 31/53A61K 31/517C07D 253/06A61P 35/00A61P 37/08A61P 9/10A61P 1/02A61P 27/02A61K 31/519Y02A50/30
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Claims
Abstract
wherein each substituent is defined as defined in the description.
Claims
exact text as granted — not AI-modified1 : A compound of Formula [I]:
wherein R 1 is
(1) C 1-8 alkyl,
(2) halo-C 1-8 alkyl,
(3) C 3-8 cycloalkyl optionally substituted with the same or different 1 to 3 substituents selected from Group A 1 , or
(4) C 3-8 cycloalkyl-C-4 alkyl wherein the C 3-8 cycloalkyl moiety may be optionally substituted with the same or different 1 to 3 substituents selected from Group A 1 ,
Group A 1 is
(1) halogen,
(2) C 1-4 alkyl, or
(3) halo-C 1-4 alkyl,
X 1 is
(1) a bond, or
(2) —O—,
R 2 is
(1) hydrogen, or
(2) halogen,
R 3 is
(1) hydrogen, or
(2) —Y 3 —COO—R 30 ,
Y 3 is
(1) C 1-8 alkylene,
(2) C 5-8 cycloalkylene,
(3) bridged C 5-8 cycloalkylene, or
(4) C 6-14 arylene,
R 30 is
(1) hydrogen, or
(2) C 1-4 alkyl,
X 2 is
(1) ═C(R 4 )—, or
(2) ═N—,
R 4 is
(1) hydrogen, or
(2) C 1-4 alkyl,
X 3 is
(1) —C(R 5 )(R 6 )—,
X 4 is
(1) a bond, or
(2) —C(R 7 )(R 8 )—,
X 5 is
(1) —C(R 9 )(R 10 )—
(2) —N(R 11 )—, or
(3) —O—,
R 5 and R 6 are each independently
(1) hydrogen,
(2) C 1-4 alkyl,
(3) halo-C 1-4 alkyl,
(4) cyano-C 1-4 alkyl, or
(5) C 1-4 alkyl substituted with one substituent selected from the group consisting of —O—R 51 , —CO—R 61 , —COO—R 52 , —N(R 71 )(R 72 ), —CO—N(R 73 )(R 74 ), —N(R 75 )—CO—R 62 , —N(R 76 )—COO—R 53 , and —O—S(O) 2 —R 63 ,
R 7 , R 8 , R 9 and R 10 are each independently
(1) hydrogen,
(2) halogen,
(3) cyano,
(4) hydroxy,
(5) C 1-4 alkyl,
(6) halo-C 1-4 alkyl,
(7) cyano-C 1-4 alkyl,
(8) C 1-4 alkoxy, or
(9) C 1-4 alkyl substituted with one substituent selected from the group consisting of —O—R 51 , —CO—R 61 , —COO—R 52 , —N(R 71 )(R 72 ), —CO—N(R 73 )(R 74 ), —N(R 75 )—CO—R 62 , —N(R 76 )—COO—R 53 , and —O—S(O) 2 —R 3 ,
R 51 , R 52 , and R 53 are each independently
(1) hydrogen,
(2) C 1-4 alkyl, or
(3) C 6-14 aryl-C 1-4 alkyl,
R 61 , R 62 , and R 63 are each independently
(1) C 1-4 alkyl,
R 71 , R 72 , R 73 , R 74 , R 75 , and R 76 are each independently
(1) hydrogen, or
(2) C 1-4 alkyl,
R 11 is
(1) —CO—R 111 , or
(2) —COO—R 112 ,
R 111 is
(1) C 1-4 alkyl, and
R 112 is
(1) C 1 -4 alkyl, or a pharmaceutically acceptable salt thereof.
2 : The compound according to claim 1 , having a structure of Formula [II]:
wherein each variable is defined as defined in claim 1 , or a pharmaceutically acceptable salt thereof.
3 : The compound according to claim 1 , wherein X 2 is ═N—, or a pharmaceutically acceptable salt thereof.
4 : The compound according to claim 1 , wherein X 2 is —C(R 4 )— and R 4 is hydrogen, or a pharmaceutically acceptable salt thereof.
5 : The compound according to claim 1 , wherein R 3 is hydrogen, or a pharmaceutically acceptable salt thereof.
6 : The compound according to claim 1 , wherein R 3 is —Y 3 —COO—R 3 ,
Y 3 is
(1) C 1-8 alkylene,
(2) Cm cycloalkylene, or
(3) bridged C 5-8 cycloalkylene, and
R 30 is hydrogen or C 1-4 alkyl, or a pharmaceutically acceptable salt thereof.
7 : The compound according to claim 1 , wherein R 2 is halogen, or a pharmaceutically acceptable salt thereof.
8 : The compound according to claim 1 , wherein R 1 is C 1-8 alkyl and X 1 is a bond, or a pharmaceutically acceptable salt thereof.
9 : The compound according to claim 1 , wherein R 5 and R 6 are each independently hydrogen or C 1-4 alkyl, or a pharmaceutically acceptable salt thereof.
10 : The compound according to claim 1 , wherein X 4 is a bond or —C(R 7 )(R 8 )— and both of R 7 and R 8 are hydrogen, or a pharmaceutically acceptable salt thereof.
11 : The compound according to claim 1 , wherein X 5 is —C(R 9 )(R 10 )— or —O— and both of R 9 and R 10 are hydrogen, or a pharmaceutically acceptable salt thereof.
12 . (canceled)
13 : A pharmaceutical composition comprising a compound according to claim 1 or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier.
14 : An RORγ antagonist comprising a compound according to claim 1 or a pharmaceutically acceptable salt thereof.
15 . (canceled)
16 : A method of antagonizing RORγ, comprising administering a therapeutically effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt thereof to a mammal.
17 : A method of treating or preventing a disease selected from the group consisting of autoimmune diseases, allergic diseases, dry eye, fibrosis, cancers, metabolic disease, ischemia, cardiomyopathy, hypertension, and periodontal disease, comprising administering a therapeutically effective amount of a compound according to claim 1 or a pharmaceutically acceptable salt thereof to a mammal.
18 - 21 . (canceled)
22 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.
23 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.
24 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.
25 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.
26 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.
27 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.
28 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.
29 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.
30 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.
31 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.
32 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.
33 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.
34 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.
35 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.
36 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.
37 : The compound according to claim 1 , having a structure:
or a pharmaceutically acceptable salt thereof.Join the waitlist — get patent alerts
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