(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.

    SUBSTITUTED BENZFUROCHROMENES AND RELATED COMPOUNDS FOR THE PREVENTION AND TREATMENT OF BONE RELATED DISORDERS
    4.
    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。

    Substituted benzfurochromenes and related compounds for the prevention and treatment of bone related disorders
    5.
    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。

    Method and apparatus for enabling collaborative product development processes
    6.
    发明授权
    Method and apparatus for enabling collaborative product development processes 有权
    用于实现协同产品开发过程的方法和设备

    公开(公告)号:US08225283B2

    公开(公告)日:2012-07-17

    申请号:US11862171

    申请日:2007-09-26

    IPC分类号: G06F9/44

    CPC分类号: G06F8/71

    摘要: A computer-implemented method supporting collaborative product development. A plurality of artifacts associated with the collaborative product development is maintained under revision control in a first repository. Each artifact has a plurality of lifecycle states and each artifact is associated with a first finite state machine (FSM) that defines lifecycle state transitions for the artifacts. A plurality of artifact tuples associated with the collaborative product development is maintained under revision control in a second repository. At least one artifact tuple is comprised of at least one access information providing access to at least one of said plurality of artifacts in the first repository. Each artifact tuple has a plurality of lifecycle states and each artifact tuple is associated with a second finite state machine (FSM) that defines lifecycle state transitions for the artifact tuples. There exists a set of lifecycle state transition mappings which maps all valid lifecycle state transitions for an artifact with desired lifecycle state transitions for an artifact tuple and all valid lifecycle state transitions for an artifact tuple with desired lifecycle state transitions for an artifact. A workflow process relating to an evolution of an artifact or artifact tuple is expressed through sequencing of one or more members of the said lifecycle state transition mappings set.

    摘要翻译: 支持协同产品开发的计算机实现方法。 与协作产品开发相关联的多个工件在第一仓库中被维护在版本控制下。 每个工件具有多个生命周期状态,并且每个工件与定义工件的生命周期状态转换的第一有限状态机(FSM)相关联。 与协作产品开发相关联的多个伪像元组在第二存储库中被维护在版本控制下。 至少一个工件元组由至少一个访问信息组成,提供对第一存储库中的所述多个工件中的至少一个工件的访问。 每个工件元组具有多个生命周期状态,并且每个工件元组与定义人造元组的生命周期状态转换的第二有限状态机(FSM)相关联。 存在一组生命周期状态转换映射,它将工件的所有有效生命周期状态转换与工件元组的所需生命周期状态转换和工件的所有生命周期状态转换的工件元组的所有有效生命周期状态转换进行映射。 通过对所述生命周期状态转换映射集合中的一个或多个成员的排序来表示与工件或伪像元组的演进有关的工作流过程。

    Techniques supporting collaborative product development
    8.
    发明授权
    Techniques supporting collaborative product development 有权
    支持协同产品开发的技术

    公开(公告)号:US07343386B2

    公开(公告)日:2008-03-11

    申请号:US11048001

    申请日:2005-01-31

    IPC分类号: G06F17/30

    摘要: A plurality of artifacts, in a plurality of repositories, are maintained under revision control. A plurality of artifact tuples, in another repository, are maintained under revision control. At least one first artifact tuple comprise first information providing access to at least one of the artifacts. At least one second artifact tuple comprises second information providing access to at least one other artifact tuple. Each of the artifact tuples are associated with at least one of a plurality of product development processes. An apparatus comprises a plurality of repositories, each maintaining under revision control a plurality of artifacts and another repository that maintains under revision control a plurality of artifact tuples. A workflow process is adapted to allow users to associate each of the artifact tuples with at least one of a plurality of product development processes.

    摘要翻译: 在多个仓库中的多个工件保持在修订控制下。 在另一个存储库中的多个伪像元组被维护在版本控制之下。 至少一个第一伪像元组包括提供对至少一个伪像的访问的第一信息。 至少一个第二伪像元组包括提供对至少一个其他伪像元组的访问的第二信息。 每个工件元组与多个产品开发过程中的至少一个相关联。 一种装置包括多个存储库,每个存储库都在修订控制下维护多个工件,另一个存储库维护着许多伪影元组的版本控制。 工作流过程适于允许用户将每个工件元组与多个产品开发过程中的至少一个相关联。

    METHOD AND APPARATUS FOR ENABLING COLLABORATIVE PRODUCT DEVELOPMENT PROCESSES
    9.
    发明申请
    METHOD AND APPARATUS FOR ENABLING COLLABORATIVE PRODUCT DEVELOPMENT PROCESSES 有权
    促进协同产品开发过程的方法和设备

    公开(公告)号:US20090083711A1

    公开(公告)日:2009-03-26

    申请号:US11862171

    申请日:2007-09-26

    IPC分类号: G06F9/44

    CPC分类号: G06F8/71

    摘要: A computer-implemented method supporting collaborative product development. A plurality of artifacts associated with the collaborative product development is maintained under revision control in a first repository. Each artifact has a plurality of lifecycle states and each artifact is associated with a first finite state machine (FSM) that defines lifecycle state transitions for the artifacts. A plurality of artifact tuples associated with the collaborative product development is maintained under revision control in a second repository. At least one artifact tuple is comprised of at least one access information providing access to at least one of said plurality of artifacts in the first repository. Each artifact tuple has a plurality of lifecycle states and each artifact tuple is associated with a second finite state machine (FSM) that defines lifecycle state transitions for the artifact tuples. There exists a set of lifecycle state transition mappings which maps all valid lifecycle state transitions for an artifact with desired lifecycle state transitions for an artifact tuple and all valid lifecycle state transitions for an artifact tuple with desired lifecycle state transitions for an artifact. A workflow process relating to an evolution of an artifact or artifact tuple is expressed through sequencing of one or more members of the said lifecycle state transition mappings set.

    摘要翻译: 支持协同产品开发的计算机实现方法。 与协作产品开发相关联的多个工件在第一仓库中被维护在版本控制下。 每个工件具有多个生命周期状态,并且每个工件与定义工件的生命周期状态转换的第一有限状态机(FSM)相关联。 与协作产品开发相关联的多个伪像元组在第二存储库中被维护在版本控制下。 至少一个工件元组由至少一个访问信息组成,提供对第一存储库中的所述多个工件中的至少一个工件的访问。 每个工件元组具有多个生命周期状态,并且每个工件元组与定义人造元组的生命周期状态转换的第二有限状态机(FSM)相关联。 存在一组生命周期状态转换映射,它将工件的所有有效生命周期状态转换与工件元组的所需生命周期状态转换和工件的所有生命周期状态转换的工件元组的所有有效生命周期状态转换进行映射。 通过对所述生命周期状态转换映射集合中的一个或多个成员的排序来表示与工件或伪像元组的演进有关的工作流过程。

    Techniques Supporting Collaborative Product Development
    10.
    发明申请
    Techniques Supporting Collaborative Product Development 审中-公开
    技术支持协同产品开发

    公开(公告)号:US20080046472A1

    公开(公告)日:2008-02-21

    申请号:US11926781

    申请日:2007-10-29

    IPC分类号: G06F17/30

    摘要: A plurality of artifacts, in a plurality of repositories, are maintained under revision control. A plurality of artifact tuples, in another repository, are maintained under revision control. At least one first artifact tuple comprise first information providing access to at least one of the artifacts. At least one second artifact tuple comprises second information providing access to at least one other artifact tuple. Each of the artifact tuples are associated with at least one of a plurality of product development processes. An apparatus comprises a plurality of repositories, each maintaining under revision control a plurality of artifacts and another repository that maintains under revision control a plurality of artifact tuples. A workflow process is adapted to allow users to associate each of the artifact tuples with at least one of a plurality of product development processes.

    摘要翻译: 在多个仓库中的多个工件保持在修订控制下。 在另一个存储库中的多个伪像元组被维护在版本控制之下。 至少一个第一伪像元组包括提供对至少一个伪像的访问的第一信息。 至少一个第二伪像元组包括提供对至少一个其他伪像元组的访问的第二信息。 每个工件元组与多个产品开发过程中的至少一个相关联。 一种装置包括多个存储库,每个存储库都在修订控制下维护多个工件,另一个存储库维护着许多伪影元组的版本控制。 工作流过程适于允许用户将每个工件元组与多个产品开发过程中的至少一个相关联。