Substituted benzfurochromenes and related compounds for the prevention and treatment of bone related disorders
    1.
    发明授权
    Substituted benzfurochromenes and related compounds for the prevention and treatment of bone related disorders 有权
    用于预防和治疗骨相关疾病的取代苯并呋喃并烯和相关化合物

    公开(公告)号:US08686028B2

    公开(公告)日:2014-04-01

    申请号:US13127913

    申请日:2009-05-14

    CPC分类号: C07D493/04 C07D311/36

    摘要: The present invention relates to novel substituted benzfurochromenes and related compounds having the general formula (I), salts and chiral, achiral derivatives thereof; wherein R1, R2, R3, R4, R5, R6, R7, R8 are independently selected from the groups consisting of hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkylthio, optionally substituted amino, optionally substituted acylamino, optionally substituted arylamino, optionally substituted acylthio, optionally substituted acyl, optionally substituted aroyl, optionally substituted acyloxy, optionally substituted thioamido, halogens, nitriles, esters, hydroxy, mercapto, carbontrifluoride, nitro but not limited to this; wherein R1R2 or R2R3 or R6R7 may be connected and form either a five membered ring or a six membered ring such as optionally substituted furan, optionally substituted dihydrofuran, optionally substituted pyran; or may be connected through a methylenedeoxy moiety; wherein X is selected from the units consisting of optionally a ketone group, optionally a methylene group, optionally substituted methylene group, optionally substituted alkene; wherein Y and Z is selected from the units consisting of CH, C—OH, C-Me, C—OMe with the proviso that bond between Y and Z is a single bond; Wherein Y and Z may be a carbon atom with the proviso that bond between Y and Z is a double bond. The compounds of the general formula is useful for the prevention and treatment of bone related disorders.

    摘要翻译: 本发明涉及具有通式(I)的新型取代的苯并呋喃和其相关化合物,其盐和手性的非手性衍生物; 其中R1,R2,R3,R4,R5,R6,R7,R8独立地选自氢,任选取代的烷基,任选取代的烯基,任选取代的烷氧基,任选取代的芳基,任选取代的杂芳基,任选取代的烷硫基, 任选取代的氨基,任选取代的酰基氨基,任选取代的芳基氨基,任选取代的酰基硫基,任选取代的酰基,任选取代的芳酰基,任选取代的酰氧基,任选取代的硫代酰氨基,卤素,腈,酯,羟基,巯基,三氟化碳,硝基,但不限于此 ; 其中R1R2或R2R3或R6R7可以连接并形成五元环或六元环,例如任选取代的呋喃,任选取代的二氢呋喃,任选取代的吡喃; 或可以通过亚甲二氧基部分连接; 其中X选自由任选的酮基,任选的亚甲基,任选取代的亚甲基,任选取代的烯烃组成的单元; 其中Y和Z选自由CH,C-OH,C-Me,C-OMe组成的单元,条件是Y和Z之间的键是单键; 其中Y和Z可以是碳原子,条件是Y和Z之间的键是双键。 通式的化合物可用于预防和治疗骨相关疾病。

    SUBSTITUTED BENZFUROCHROMENES AND RELATED COMPOUNDS FOR THE PREVENTION AND TREATMENT OF BONE RELATED DISORDERS
    2.
    发明申请
    SUBSTITUTED BENZFUROCHROMENES AND RELATED COMPOUNDS FOR THE PREVENTION AND TREATMENT OF BONE RELATED DISORDERS 有权
    用于预防和治疗骨髓相关疾病的替代苯唑西林和相关化合物

    公开(公告)号:US20120003273A1

    公开(公告)日:2012-01-05

    申请号:US13127913

    申请日:2009-05-14

    CPC分类号: C07D493/04 C07D311/36

    摘要: The present invention relates to novel substituted benzfurochromenes and related compounds having the general formula (I), salts and chiral, achiral derivatives thereof; wherein R1, R2, R3, R4, R5, R6, R7, R8 are independently selected from the groups consisting of hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkoxyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted alkylthio, optionally substituted amino, optionally substituted acylamino, optionally substituted arylamino, optionally substituted acylthio, optionally substituted acyl, optionally substituted aroyl, optionally substituted acyloxy, optionally substituted thioamido, halogens, nitriles, esters, hydroxy, mercapto, carbontrifluoride, nitro but not limited to this; wherein R1R2 or R2R3 or R6R7 may be connected and form either a five membered ring or a six membered ring such as optionally substituted furan, optionally substituted dihydrofuran, optionally substituted pyran; or may be connected through a methylenedeoxy moiety; wherein X is selected from the units consisting of optionally a ketone group, optionally a methylene group, optionally substituted methylene group, optionally substituted alkene; wherein Y and Z is selected from the units consisting of CH, C—OH, C-Me, C—OMe with the proviso that bond between Y and Z is a single bond; Wherein Y and Z may be a carbon atom with the proviso that bond between Y and Z is a double bond. The compounds of the general formula is useful for the prevention and treatment of bone related disorders.

    摘要翻译: 本发明涉及具有通式(I)的新型取代的苯并呋喃和其相关化合物,其盐和手性的非手性衍生物; 其中R1,R2,R3,R4,R5,R6,R7,R8独立地选自氢,任选取代的烷基,任选取代的烯基,任选取代的烷氧基,任选取代的芳基,任选取代的杂芳基,任选取代的烷硫基, 任选取代的氨基,任选取代的酰基氨基,任选取代的芳基氨基,任选取代的酰基硫基,任选取代的酰基,任选取代的芳酰基,任选取代的酰氧基,任选取代的硫代酰氨基,卤素,腈,酯,羟基,巯基,三氟化碳,硝基,但不限于此 ; 其中R1R2或R2R3或R6R7可以连接并形成五元环或六元环,例如任选取代的呋喃,任选取代的二氢呋喃,任选取代的吡喃; 或可以通过亚甲二氧基部分连接; 其中X选自由任选的酮基,任选的亚甲基,任选取代的亚甲基,任选取代的烯烃组成的单元; 其中Y和Z选自由CH,C-OH,C-Me,C-OMe组成的单元,条件是Y和Z之间的键是单键; 其中Y和Z可以是碳原子,条件是Y和Z之间的键是双键。 通式的化合物可用于预防和治疗骨相关疾病。

    (3R, 4R)-trans-3, 4-diarylchroman derivatives and a method for the prevention and/or treatment of estrogen dependent diseases

    公开(公告)号:US07427686B2

    公开(公告)日:2008-09-23

    申请号:US10677116

    申请日:2003-09-30

    IPC分类号: C07D311/00

    CPC分类号: C07D311/58

    摘要: The present invention relates to compounds of the formula I in which substituents R2 and R3 are arranged in trans-configuration: wherein: R1 is H or C1-C6 alkyl; C3-C7 cycloalkyl; R2 is phenyl, optionally substituted with 1 to 5 substituents independently selected from the group comprising OH, C1-C6-alkyl, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkoxy and phenyl, wherein R4 is C1-C6 alkyl; R3 is phenyl substituted with OR5 wherein R5 has the formula (II), (III) or (IV) wherein Y is chosen from NHR4, NR42, NHCOR4, NHSO2R4, CONHR4, CONR4, CONR42, COOH, COOR4, SO2R4, SOR4, SONHR4, SONR42, a C3-C7 heterocyclic ring, saturated or unsaturated, containing one or two heteroatoms independently selected from the group consisting of O, S and N, optionally being substituted with 1 to 3 substituents independently selected from the group comprising H, OH, halogen, nitro, cyano, SH, SR4, trihalo-C1-C6-alkyl, C1-C6-alkyl and C1-C6-alkoxy, preferably NHR4, NR24, or a nitrogen heterocycle, wherein R4 is as defined above, and the esters, ethers, and salts of the compounds of formula I, optionally along pharmaceutically acceptable excipients, a process for the preparation of the same, and a method of preventing and/or treating estrogen-related disease conditions in a subject using compounds of formula 1, or its salts, optionally along with pharmaceutically acceptable excipients.