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公开(公告)号:US09011885B2
公开(公告)日:2015-04-21
申请号:US14447434
申请日:2014-07-30
发明人: Jean Hilaire Saurat
IPC分类号: A61K9/00 , A61K31/00 , A61K31/407 , A61K31/352
CPC分类号: A61K31/352 , A61K9/0014 , A61K31/00 , A61K31/407
摘要: The use, as a dermatological or cosmetic medicament, of compounds capable of transiently interacting with the AhR receptor (aryl hydrocarbon receptor) as agents for modulating skin functions such as sebaceous function, skin healing, skin atrophy termed “dermatoporosis”, estrogen deprivation and defense against infection, without inducing other toxic effects of the TCDD type.The compounds that interact with the AhR receptor are chosen in that they have a metabolism favorable to the dissociation of these effects, in particular by virtue of in situ production from a precursor and/or metabolization modulated in situ.
摘要翻译: 使用能够与AhR受体(芳烃受体)瞬时相互作用的化合物作为皮肤病学或化妆品药物,用作调节皮肤功能如皮脂腺功能,皮肤愈合,称为“皮肤病”的皮肤萎缩,雌激素剥夺和防御 免受感染,不引起TCDD类型的其他毒性作用。 选择与AhR受体相互作用的化合物,因为它们具有有利于这些作用的解离的代谢,特别是通过原位原位产生和/或原位调节的代谢。
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公开(公告)号:US20150005373A1
公开(公告)日:2015-01-01
申请号:US14447434
申请日:2014-07-30
发明人: Jean Hilaire Saurat
IPC分类号: A61K9/00 , A61K31/352
CPC分类号: A61K31/352 , A61K9/0014 , A61K31/00 , A61K31/407
摘要: The use, as a dermatological or cosmetic medicament, of compounds capable of transiently interacting with the AhR receptor (aryl hydrocarbon receptor) as agents for modulating skin functions such as sebaceous function, skin healing, skin atrophy termed “dermatoporosis”, estrogen deprivation and defense against infection, without inducing other toxic effects of the TCDD type.The compounds that interact with the AhR receptor are chosen in that they have a metabolism favorable to the dissociation of these effects, in particular by virtue of in situ production from a precursor and/or metabolization modulated in situ.
摘要翻译: 使用能够与AhR受体(芳烃受体)瞬时相互作用的化合物作为皮肤病学或化妆品药物,用作调节皮肤功能如皮脂腺功能,皮肤愈合,称为“皮肤病”的皮肤萎缩,雌激素剥夺和防御 免受感染,不引起TCDD类型的其他毒性作用。 选择与AhR受体相互作用的化合物,因为它们具有有利于这些作用的解离的代谢,特别是通过原位原位产生和/或原位调节的代谢。
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公开(公告)号:US20180118707A1
公开(公告)日:2018-05-03
申请号:US15735053
申请日:2016-06-07
发明人: Nigel Robert Arnold Beeley , Howard Glenn Welgus , Jay Edward Birnbaum , J. Gordon Foulkes , Celia Patricia Jenkinson , Jean Hilaire Saurat
IPC分类号: C07D311/80 , A61P17/00 , A61K9/00 , A61P17/08 , A61P17/10 , A61P23/02 , A61P29/00 , A61P19/02 , A61P1/04 , A61P19/04 , A61P17/06 , A61P11/06 , A61P37/06 , A61P25/28 , A61P25/00 , A61P3/00 , A61P3/04 , A61K31/352 , C07D407/04 , A61K31/357 , C07D493/04 , C07D405/04 , A61K31/4433 , C07D491/056 , A61K31/4355 , A61K31/436
CPC分类号: C07D311/80 , A61K9/0014 , A61K31/352 , A61K31/357 , A61K31/36 , A61K31/4355 , A61K31/436 , A61K31/4433 , A61P1/04 , A61P3/00 , A61P3/04 , A61P11/06 , A61P17/00 , A61P17/06 , A61P17/08 , A61P17/10 , A61P19/02 , A61P19/04 , A61P23/02 , A61P25/00 , A61P25/28 , A61P29/00 , A61P37/06 , C07B2200/07 , C07B2200/09 , C07D405/04 , C07D407/04 , C07D491/056 , C07D493/04
摘要: The present invention provides compounds of the following structure, methods of using such compounds, and pharmaceutical compositions containing such compounds. In addition, this invention provides methods for the treatment and/or prevention of disease states mediated by Aryl Hydrocarbon receptor pathways.
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公开(公告)号:US20160200735A1
公开(公告)日:2016-07-14
申请号:US14995556
申请日:2016-01-14
发明人: Stephen D. Barrett , James B. Kramer , Mark L. Boys , Huifen Chen
IPC分类号: C07D495/04
CPC分类号: C07D495/04 , A61K9/0014 , A61K31/4365
摘要: The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as therapeutic agents in the treatment of TGFβ-mediated conditions, including cancer and fibrotic disorders. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
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公开(公告)号:US09358220B2
公开(公告)日:2016-06-07
申请号:US14607597
申请日:2015-01-28
发明人: Jean Hilaire Saurat
IPC分类号: A61K9/00 , A61K31/352 , A61K31/00 , A61K31/407
CPC分类号: A61K31/352 , A61K9/0014 , A61K31/00 , A61K31/407
摘要: The use, as a dermatological or cosmetic medicament, of compounds capable of transiently interacting with the AhR receptor (aryl hydrocarbon receptor) as agents for modulating skin functions such as sebaceous function, skin healing, skin atrophy termed “dermatoporosis”, estrogen deprivation and defense against infection, without inducing other toxic effects of the TCDD type.The compounds that interact with the AhR receptor are chosen in that they have a metabolism favorable to the dissociation of these effects, in particular by virtue of in situ production from a precursor and/or metabolization modulated in situ.
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公开(公告)号:US09938289B2
公开(公告)日:2018-04-10
申请号:US14995556
申请日:2016-01-14
发明人: Stephen D. Barrett , James B. Kramer , Mark L. Boys , Huifen Chen
IPC分类号: C07D495/04 , A61K9/14 , A61K31/4365 , A61K9/00
CPC分类号: C07D495/04 , A61K9/0014 , A61K31/4365
摘要: The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as therapeutic agents in the treatment of TGFβ-mediated conditions, including cancer and fibrotic disorders. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
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公开(公告)号:US20150216840A1
公开(公告)日:2015-08-06
申请号:US14607597
申请日:2015-01-28
发明人: Jean Hilaire Saurat
IPC分类号: A61K31/352 , A61K9/00
CPC分类号: A61K31/352 , A61K9/0014 , A61K31/00 , A61K31/407
摘要: The use, as a dermatological or cosmetic medicament, of compounds capable of transiently interacting with the AhR receptor (aryl hydrocarbon receptor) as agents for modulating skin functions such as sebaceous function, skin healing, skin atrophy termed “dermatoporosis”, estrogen deprivation and defense against infection, without inducing other toxic effects of the TCDD type.The compounds that interact with the AhR receptor are chosen in that they have a metabolism favorable to the dissociation of these effects, in particular by virtue of in situ production from a precursor and/or metabolization modulated in situ.
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公开(公告)号:US08980936B2
公开(公告)日:2015-03-17
申请号:US13945622
申请日:2013-07-18
发明人: Jin Li , Nicole Lee Kolosko
IPC分类号: A61K31/4025 , C07D207/12 , C07D207/24
CPC分类号: C07D207/12 , A61K31/4025 , C07D207/24
摘要: The present invention is directed to the compound 2-(4-(hydroxymethyl)phenoxy)-1-(3-(2-(trifluoromethyl)phenoxy)pyrrolidin-1-yl)ethanone, its use as an inhibitor of stearoyl CoA desaturase and to pharmaceutical compositions containing this compound.
摘要翻译: 本发明涉及化合物2-(4-(羟甲基)苯氧基)-1-(3-(2-(三氟甲基)苯氧基)吡咯烷-1-基)乙酮,其用作硬脂酰CoA去饱和酶的抑制剂, 含有该化合物的药物组合物。
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公开(公告)号:US09260450B2
公开(公告)日:2016-02-16
申请号:US14637097
申请日:2015-03-03
发明人: Stephen D. Barrett , James B. Kramer , Mark L. Boys , Huifen Chen
IPC分类号: C07D495/04 , A61K31/4365 , A61K9/00
CPC分类号: C07D495/04 , A61K9/0014 , A61K31/4365
摘要: The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as therapeutic agents in the treatment of TGFβ-mediated conditions, including cancer and fibrotic disorders. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
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公开(公告)号:US09090625B2
公开(公告)日:2015-07-28
申请号:US13864457
申请日:2013-04-17
发明人: Stephen D. Barrett , James B. Kramer , Mark L. Boys , Huifen Chen
IPC分类号: A61K31/4365 , C07D495/04
CPC分类号: C07D495/04 , A61K9/0014 , A61K31/4365
摘要: The present invention provides for compounds of Formula I, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined therefor in the specification, and pharmaceutically acceptable salts thereof, that are useful as therapeutic agents in the treatment of TGFβ-mediated conditions, including cancer and fibrotic disorders. Also provided are pharmaceutical compositions comprising one or more compounds of Formula I.
摘要翻译: 本发明提供式I化合物及其药学上可接受的盐,其中R 1,R 2,R 3,R 4,R 5,R 6和R 7具有本说明书中定义的任何值及其药学上可接受的盐, 可用作治疗TGF-bgr介导的病症,包括癌症和纤维化疾病的治疗剂。 还提供了包含一种或多种式I化合物的药物组合物。
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