01-03-2018 дата публикации
Номер: US20180057505A1
Автор:
Bubenik Monica,
Dietrich Evelyne,
Fournier Pierre-Andre,
Lacoste Jean-Eric,
Lessard Stephanie,
Martel Julien,
Ramtohul Yeeman,
Sayegh Camil Elie,
St-Onge Miguel,
STURINO Claudio,
Szychowski Janek,
Vallee Frederic
Принадлежит:
The compounds of formula I, wherein the variables are as defined herein, and pharmaceutically acceptable salts thereof are useful as inhibitors of the PAR-2 signaling pathway. The compounds of formula I and pharmaceutically acceptable compositions comprising such compounds can be employed for treating various diseases, disorders, and conditions. 3. The compound of or , wherein Z is —NX—.4. The compound of claim 3 , wherein J is methyl.5. The compound of any one of - claim 3 , wherein p is 1 or 2.6. The compound of any one of - claim 3 , wherein n is 1.14. The compound of any one of - claim 3 , wherein Ris —(V)—Y: wherein{'sub': 1-6', '1-6', '2', '1-4', '2', '1-4, 'V is Caliphatic wherein up to three carbon units of said Caliphatic can each be optionally and independently replaced with —O—, —NR—, —S—, —C(O)—, or —S(O); wherein V is optionally substituted with 1-3 occurrences of halogen, Calkyl, OH, NH, or —NRC(O)Calkyl; and'}{'sup': 'Y', 'Y is H, cyclopropyl, cyclobutyl, cyclopentyl, cxyclohexyl, oxetanyl, azetidinyl, tetrahydrofuranyl, pyrrolidinyl, tetrahydropyranyl, piperidinyl, piperazinyl, thiomorpholinyl, morpholinyl, imidazolyl, isoxazolyl, pyrazolyl, pyridinyl, pyrazinyl, pyridazinyl, phenyl, oxadiazolyl, thienyl, pyrimidinyl, triazolyl, tetrazolyl, oxazolyl, thiazolyl, spiro[3,3]hepatanyl, or 1,1-dioxide-isothiazolidinyl; wherein Y is optionally and independently substituted with 1-4 occurrences of J;'}{'sup': 'Y', 'sub': 1-4', '1-4', '1-4', '1-4', '1-4', '2', '2', '1-4', '2', '2', 't', '2', 't', '1-2', '1-2', 't', '1-2', 't', '1-2', '1-2', '2', 't', '1-2', '2', 't', '1-2', '2', '2, 'Jis H, oxo, CN, halogen, Calkyl, haloCalkyl, —OH, —O(Calkyl), NH(Calkyl), N(Calkyl), S(O)(Calkyl), phenyl, NH, tetrazole, (CH)—C(O)OH, (CH)—C(O)O(Calkyl), (CH(Calkyl))—C(O)OH, (CH(Calkyl))—C(O)O(Calkyl), (C(Calkyl))—C(O)OH, (C(Calkyl))—C(O)O(Calkyl), or —C(O)O—CH—O—P(O)(OH);'}a is 0 or 1; andeach t is independently 0 or 1.15. The compound of any one of - claim 3 , wherein Ris —( ...
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