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    Isoxazole o-linked carbamoyl cyclohexyl acids as LPA antagonists
    31.
    发明授权
    Isoxazole o-linked carbamoyl cyclohexyl acids as LPA antagonists 有权

    公开(公告)号：US11180488B2

    公开(公告)日：2021-11-23

    申请号：US16954546

    申请日：2018-12-18

    Applicant: BRISTOL-MYERS SQUIBB COMPANY

    Inventor： Peter Tai Wah Cheng ,  Robert F. Kaltenbach, III ,  Hao Zhang ,  Yan Shi ,  Jun Li

    IPC: C07D413/04 ,  C07D261/08 ,  C07D413/12

    Abstract: The present invention provides compounds of Formula (Ia) or (Ib) or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein X1, X2, X3, and X4 are each independently CR6 or N; provided that no more than two of X1, X2, X3, or X4 are N; L is C1-4 alkylene substituted with 0 to 4 R7; R1 is (—CH2)aR9; a is an integer of 0 or 1; R2 is each independently halo, cyano, hydroxyl, amino, C1-6 alkyl, C3-6 cycloalkyl, C4-6 heterocyclyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxy, alkoxyalkyl, haloalkoxyallcyl, or haloalkoxy; n is an integer of 0, 1, or 2; R3 is hydrogen, C1-6 alkyl, C1-6 deuterated alkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, or haloalkoxy, and the alkyl, by itself or as part of other moiety, is optionally substituted with deuterium partially or fully; R4 is C1-10 alkyl, C1-10 deuterated alkyl, C1-10 haloalkyl, C1-10 alkenyl, C3-8 cycloalkyl, 6 to 10-membered aryl, 3 to 8-membered heterocyclyl, —(C1-6 alkylene)-(C3-8 cycloalkyl), —(C1-6 alkylene)-(6 to 10-membered aryl), —(C1-6 alkylene)-(3 to 8-membered heterocyclyl), or —(C1-6 alkylene)-(5 to 6-membered heteroaryl); wherein each of the alkyl, alkylene, alkenyl, cycloalkyl, aryl, heterocyclyl, and heteroaryl, by itself or as part of other moiety, is independently substituted with 0 to 3 R8; or alternatively, R3 and R4, taken together with the N atom to which they are attached, form a 4 to 9-membered heterocyclic ring moiety which is substituted with 0 to 3 R; R5 and R6 are each independently hydrogen, halo, cyano, hydroxyl, amino, C1-6 alkyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, or haloalkoxy; R7 is halo, oxo, cyano, hydroxyl, amino, C1-6 alkyl, C3-6 cycloalkyl, C4-6 heterocyclyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, or haloalkoxy; R8 are each independently deuterium, halo, hydroxyl, amino, cyano, C1-6 alkyl, C1-6 deuterated alkyl, C2-6 alkenyl, C2-6 alkynyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, haloalkoxy, phenyl, or 5 to 6-membered heteroaryl; or alternatively, two R8, taken together with the atoms to which they are attached, form a 3 to 6-membered carbocyclic ring or a 3 to 6-membered heterocyclic ring each of which is independently substituted with 0 to 3 R12; R9 is selected from —CN, —C(O)OR10, —C(O)NR11aR11b, —CO—NH—CO—Re, —CO—NH—SO2—Re, —CO—NH—SO—Re, —SO2—OH, —SO2—NH—CO—Re, —P(O)(OH)2, tetrazol-5-yl, —CH2—CO—NH—CO—Re, —CH2—CO—NH—SO2—Re, CH2—CO—NH—SO—Re, —CH2—SO2—OH, —CH2—SO2—NH—CO—Re, —CH2—P(O)(OH)2, tetrazol-5-ylmethylene; Re is C1-6 alkyl, C3-6 cycloalkyl, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, or haloalkoxyalkyl; R10 is hydrogen or C1-10 alkyl; and R11a and R11b are each independently hydrogen, C1-6 alkyl, C3-6 cycloalkyl, C4-6 heterocyclyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, or haloalkoxy; and R12 is halo, cyano, hydroxyl, amino, C1-6alkyl, alkylamino, haloalkyl, hydroxyalkyl, aminoalkyl, alkoxyalkyl, haloalkoxyalkyl, alkoxy, haloalkoxy, phenyl, or 5 to 6-membered heteroaryl. These compounds are selective LPA receptor inhibitors.

    ISOTOPICALLY LABELED TRIAZOLOPYRIDINE 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS
    36.
    发明申请
    ISOTOPICALLY LABELED TRIAZOLOPYRIDINE 11-BETA HYDROXYSTEROID DEHYDROGENASE TYPE I INHIBITORS 审中-公开
    同位素标记的三唑基吡啶11-羟基脱氢酶脱氢酶I型抑制剂

    公开(公告)号：US20160257680A1

    公开(公告)日：2016-09-08

    申请号：US15031301

    申请日：2014-10-21

    Applicant: BRISTOL-MYERS SQUIBB COMPANY

    Inventor： Yaofeng Cheng ,  Weiqi Chen ,  Brad D. Maxwell ,  Bach D. Tran ,  Jun Li

    IPC: C07D471/04 ,  A61K31/437

    CPC classification number: C07D471/04 ,  A61K31/437 ,  C07B59/002 ,  C07B2200/05

    Abstract: Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11-beta-hydroxysteroid dehydrogenase type I inhibitor therapy. These novel compounds of formula I: or stereoisomers or pharmaceutically acceptable salts thereof, wherein R* is an isotopically labeled hydroxypropyl moiety.

    Abstract translation: 提供了新的化合物，其为11-β-羟基类固醇脱氢酶I型抑制剂。 11-β-羟基类固醇脱氢酶I型抑制剂可用于治疗，预防或减缓需要11-β-羟基类固醇脱氢酶I型抑制剂治疗的疾病进展。 这些新的式I化合物或其立体异构体或其药学上可接受的盐，其中R *是同位素标记的羟丙基部分。

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