US2023145481A1PendingUtilityA1
Substituted benzenecarboxamides as il-17a modulators
Est. expirySep 16, 2039(~13.2 yrs left)· nominal 20-yr term from priority
Inventors:Paul R. FathereeMartin S. LinsellJohn R. JacobsenWouter A. Van Der LindenTimothy J. ChurchClaudio AquinoMargot Paulick
C07D 417/12A61K 31/496C07D 405/12C07D 413/12C07D 471/04C07D 451/02C07D 241/04C07D 239/32C07D 285/06C07D 403/14C07D 487/04C07D 403/12C07D 401/12C07D 307/82C07D 493/04C07D 211/46C07D 409/14C07D 487/10C07D 491/048C07D 455/02C07D 409/12C07D 295/135C07D 401/14C07D 413/14C07D 317/48A61P 35/00C07D 231/12C07D 495/04C07D 498/04C07D 261/18C07D 279/12C07D 231/56C07D 417/14C07D 405/14C07D 333/60C07D 413/04A61P 29/00C07D 271/08
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Claims
Abstract
The disclosure herein provides compounds and pharmaceutical compositions of the structure of Formula I:for the modulation of IL-17A, useful for the treatment of inflammatory conditions, such as psoriasis.
Claims
exact text as granted — not AI-modifiedWhat is claimed is:
1 . A compound represented by the structure of Formula ID:
or a pharmaceutically acceptable salt thereof wherein:
is selected from pyrazole, tetrazole, oxadiazole, isoxazole, pyrrole, and furan any one of which is optionally substituted with one or more substituents independently selected from halogen,
—OR 11 , —N(R 11 ) 2 , —N(R 11 )S(O) 2 R 11 , —NO 2 , —CN, C 1-6 alkyl, —C 1-6 alkyl-C 3-5 carbocycle, C 3-5 carbocycle, and 3- to 5-membered heterocycle;
is selected from cyclopentyl, cyclohexyl, and cycloheptyl each of which is optionally substituted with one or more substituents independently selected from halogen, —OR 12 , and optionally substituted C 1-3 alkyl;
R 4 is
wherein
is selected from azetidine, piperidine, piperazine, morpholine, thiomorpholine, thiomorpholine 1,1-dioxide, and azaspiro[3.3]heptane any of which is optionally substituted with one or more substituents independently selected from halogen,
—OR 13 , and optionally substituted C 1-3 alkyl;
R B is selected from hydrogen, —OMe, —OEt, —CF 3 , —CHF 2 , —CH 2 F, methyl, ethyl, propyl, and isopropyl;
R′ and R″ are each halogen;
R 1 is selected from —N(R 21 )C(O)R 22 , —N(R 21 )C(O)OR 22 , and —N(R 21 )C(O)N(R 21 )(R 22 );
R 21 is independently selected at each occurrence from hydrogen and C 1-3 alkyl optionally substituted by one or more substituents independently selected from halogen, —OR 17 , —N(R 17 ) 2 , and —CN;
R 22 is selected from C 1-4 alkyl and C 3-5 carbocycle, each of which is optionally substituted with one or two substituents independently selected from halogen, —OR 18 , —SR 18 , —N(R 18 ) 2 , —C(O)R 18 , —C(O)OR 18 , C 3-10 carbocycle and 3- to 10-membered heterocycle; wherein the C 3-10 carbocycle and 3- to 10-membered heterocycle are each optionally substituted with one or more substituents selected from: halogen, —OR 18 , and —NO 2 ;
R 11 , R 12 , R 13 , R 17 , and R 18 are independently selected at each occurrence from:
hydrogen;
C 1-6 alkyl optionally substituted with one or more substituents independently selected from halogen, —OH, —O—C 1 -C 6 alkyl, —O—C 1 -C 6 haloalkyl —NH 2 , —NO 2 , ═O, —CN, C 3-10 carbocycle and 3- to 10-membered heterocycle; wherein the C 3-10 carbocycle and 3- to 10-membered heterocycle are each optionally substituted with one or more substituents selected from: halogen, —OH, —O—C 1 -C 6 alkyl, —O—C 1 -C 6 haloalkyl —NH 2 , —NO 2 , ═O, and —CN; and
C 3-12 carbocycle and 3- to 12-membered heterocycle, each of which is optionally substituted with one or more substituents independently selected from:
halogen, —OH, —O—C 1 -C 6 alkyl, —O—C 1 -C 6 haloalkyl —NH 2 , —NO 2 , ═O, —CN; and
C 1-6 alkyl optionally substituted with one or more substituents independently selected from halogen, —OH, —O—C 1 -C 6 alkyl, —O—C 1 -C 6 haloalkyl —NH 2 , —NO 2 , ═O, and —CN; and
n is 0.
2 . The compound or salt of claim 1 , wherein
is selected from pyrazole, oxadiazole, isoxazole, and pyrrole, each of which is optionally substituted with one or more substituents independently selected from C 1-6 alkyl, C 3-5 carbocycle, and —C 1-3 alkyl-C 3-5 carbocycle.
3 . The compound or salt of claim 1 , wherein
is selected from cyclohexyl and cycloheptyl, each of which is optionally substituted with one or more substituents independently selected from halogen and C 1-3 alkyl.
4 . The compound or salt of claim 1 , wherein
is selected from piperidine and piperazine, each of which is optionally substituted with one or more substituents independently selected from —OR 13 and C 1-3 alkyl.
5 . The compound or salt of claim 1 , wherein R B is selected from methyl, —CF 3 , —CHF 2 , and —CH 2 F.
6 . The compound or salt of claim 1 , wherein R 1 is selected from —N(R 21 )C(O)R 22 and —N(R 21 )C(O)N(R 21 )(R 22 ).
7 . The compound or salt of claim 1 , wherein R 21 is selected from hydrogen and C 1-3 alkyl.
8 . The compound or salt of claim 1 , wherein R 22 is selected from C 1-4 alkyl and C 3-5 carbocycle, each of which is optionally substituted with one or two substituents independently selected from halogen and C 3-6 carbocycle.
9 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
10 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
11 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
12 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
13 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
14 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
15 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
16 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
17 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
18 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
19 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
20 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
21 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
22 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
23 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
24 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
25 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
26 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
27 . The compound of claim 1 , wherein the compound is represented by the following structure:
or a salt thereof.
28 . A pharmaceutical composition comprising a pharmaceutically acceptable excipient and a compound or salt of claim 1 .
29 . A method of inhibiting IL-17A in a subject in a subject in need thereof, comprising administering to the subject in need thereof a compound or salt of claim 1 .
30 . A method of treating an inflammatory disease or condition selected from plaque psoriasis, guttate psoriasis, inverse psoriasis, pustular psoriasis, erythrodermic psoriasis, aspsoriatic arthritis, ankyslosing spondylitis, hidradenitis suppurutiva, rheumatoid arthritis, Palmoplantar Psoriasis, Spondyloarthritis, and Non-infectious Uveitis, comprising administering to a subject in need thereof a compound or salt of claim 1 .Cited by (0)
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