EP2797889A4 - Neuartige arylalkenderivate und deren verwendung als selektive östrogenrezeptormodulatoren - Google Patents

Neuartige arylalkenderivate und deren verwendung als selektive östrogenrezeptormodulatoren

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Publication number
EP2797889A4
EP2797889A4 EP12863580.2A EP12863580A EP2797889A4 EP 2797889 A4 EP2797889 A4 EP 2797889A4 EP 12863580 A EP12863580 A EP 12863580A EP 2797889 A4 EP2797889 A4 EP 2797889A4
Authority
EP
European Patent Office
Prior art keywords
novel
estrogen receptor
receptor modulators
selective estrogen
arylalkene
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP12863580.2A
Other languages
English (en)
French (fr)
Other versions
EP2797889A1 (de
Inventor
Dengming Xiao
Li Zhu
Yuandong Hu
Rong Yu
Wei Hu
Na Zhao
Yong Peng
Hong Luo
Yongxin Han
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Centaurus Biopharma Co Ltd
Original Assignee
Centaurus Biopharma Co Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from CN2011104578981A external-priority patent/CN102584687A/zh
Priority claimed from CN2011104561181A external-priority patent/CN102532073A/zh
Application filed by Centaurus Biopharma Co Ltd filed Critical Centaurus Biopharma Co Ltd
Publication of EP2797889A1 publication Critical patent/EP2797889A1/de
Publication of EP2797889A4 publication Critical patent/EP2797889A4/de
Withdrawn legal-status Critical Current

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    • C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C217/06—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted
    • C07C217/14—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring
    • C07C217/18—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted
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    • C07C215/48—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by hydroxy groups
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    • C07C217/14—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring
    • C07C217/18—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted
    • C07C217/20—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to a carbon atom of a six-membered aromatic ring the six-membered aromatic ring or condensed ring system containing that ring being further substituted by halogen atoms, by trihalomethyl, nitro or nitroso groups, or by singly-bound oxygen atoms
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EP12863580.2A 2011-12-30 2012-12-28 Neuartige arylalkenderivate und deren verwendung als selektive östrogenrezeptormodulatoren Withdrawn EP2797889A4 (de)

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CN2011104578981A CN102584687A (zh) 2011-12-30 2011-12-30 作为选择性雌激素受体调节剂的乙烯衍生物
CN2011104561181A CN102532073A (zh) 2011-12-30 2011-12-30 作为选择性雌激素受体调节剂的乙烯衍生物
US201261646628P 2012-05-14 2012-05-14
US201261646668P 2012-05-14 2012-05-14
PCT/CN2012/087884 WO2013097773A1 (en) 2011-12-30 2012-12-28 Novel arylalkene derivatives and use thereof as selective estrogen receptor modulators

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Families Citing this family (16)

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KR102134171B1 (ko) 2014-10-24 2020-07-15 란도스 바이오파마, 인크. 란티오닌 합성효소 c-유사 2-계 치료제
US10759791B2 (en) 2014-11-04 2020-09-01 Northwestern University Mammalian and bacterial nitric oxide synthase inhibitors
DE102015222031A1 (de) * 2015-11-10 2017-05-11 Robert Bosch Gesellschaft Für Medizinische Forschung Mbh Synthese von (Z)-Endoxifenhydrochlorid
CN108884079B (zh) * 2016-02-15 2021-03-05 赛诺菲 作为雌激素受体调节剂的6，7-二氢-5h-苯并[7]轮烯衍生物
WO2018091153A1 (en) 2016-11-17 2018-05-24 Sanofi Novel substituted n-(3-fluoropropyl)-pyrrolidine compounds, processes for their preparation and therapeutic uses thereof
CN108333349A (zh) * 2017-01-19 2018-07-27 浙江东方基因生物制品股份有限公司 一种4-甲基甲卡西酮人工抗原以及制备方法和运用
EP3434272A1 (de) 2017-07-25 2019-01-30 Sanofi Kombination aus palbociclib und 6-(2,4-dichlorophenyl)-5-[4-[(3s)-1-(3-fluoropropyl)pyrrolidin-3-yl]oxyphenyl]-8,9-dihydro-7h-benzo[7]annulen-2-carboxylsäure
CN107674051B (zh) * 2017-09-20 2021-01-08 南京医科大学 4-羟基他莫昔酚环状衍生物乏氧活化前药及其药物用途
WO2019108418A1 (en) 2017-11-30 2019-06-06 Landos Biopharma, Inc. Therapies with lanthionine c-like protein 2 ligands and cells prepared therewith
CN108514539B (zh) * 2018-07-11 2021-07-27 广州市腾宇化妆品有限公司 一种基于温和效果化妆品用防腐组合物及该化妆品制备方法
WO2020025574A1 (en) * 2018-08-03 2020-02-06 Bayer Aktiengesellschaft Process for the preparation of 6-(haloalkyl)-2-halo-5-acylpyridines and intermediates for this process
AR116300A1 (es) 2018-09-07 2021-04-21 Sanofi Sa Proceso para la preparación de 6-(2,4-diclorofenil)-5-[4-[(3s)-1-(3-fluoropropil)pirrolidin-3-il]oxifenil]-8,9-dihidro-7h-benzo[7]anuleno-2-carboxilato de metilo
CN117050002A (zh) 2018-11-21 2023-11-14 冰洲石生物科技公司 具有雌激素受体α降解活性的新型化合物及其用途
KR20230026522A (ko) 2019-12-20 2023-02-24 란도스 바이오파마, 인크. 란티오닌 c-유사 단백질 2 리간드, 이로 제조된 세포, 및 이를 사용하는 치료법
WO2021133886A1 (en) 2019-12-23 2021-07-01 Accutar Biotechnology Combinations of estrogen receptor degraders and cyclin-dependent kinase inhibitors for treating cancer
AU2021283577A1 (en) * 2020-06-02 2023-01-19 Chengdu Kanghong Pharmaceutical Co., Ltd. Novel thyroid hormone β receptor agonist

Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0260066A1 (de) * 1986-09-11 1988-03-16 National Research Development Corporation Tamoxifenderivate
WO1999007668A1 (en) * 1994-04-25 1999-02-18 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
WO2001036360A1 (en) * 1999-11-16 2001-05-25 Hormos Medical Corporation Triphenylalkene derivatives and their use as selective estrogen receptor modulators
WO2002066415A2 (en) * 2001-02-20 2002-08-29 The Provost, Fellows And Scholars Of The College Of The Holy And Undivided Trinity Of Queen Elizabeth Near Dublin Non-steroidal modulators of estrogen receptors
WO2005033056A2 (en) * 2003-10-08 2005-04-14 Smithkline Beecham Corporation Triphenylethylene compounds as selective estrogen receptor modulators
WO2007062148A2 (en) * 2005-11-22 2007-05-31 Smithkline Beecham Corporation Chemical compounds
WO2007062190A2 (en) * 2005-11-22 2007-05-31 Smithkline Beecham Corporation Chemical compounds
WO2007062145A2 (en) * 2005-11-22 2007-05-31 Smithkline Beecham Corporation Chemical compounds
WO2007062151A2 (en) * 2005-11-22 2007-05-31 Smithkline Beecham Corporation Chemical compounds

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102532073A (zh) * 2011-12-30 2012-07-04 北京赛林泰医药技术有限公司 作为选择性雌激素受体调节剂的乙烯衍生物
CN102584687A (zh) * 2011-12-30 2012-07-18 北京赛林泰医药技术有限公司 作为选择性雌激素受体调节剂的乙烯衍生物

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0260066A1 (de) * 1986-09-11 1988-03-16 National Research Development Corporation Tamoxifenderivate
WO1999007668A1 (en) * 1994-04-25 1999-02-18 Glaxo Wellcome Inc. Non-steroidal ligands for the estrogen receptor
WO2001036360A1 (en) * 1999-11-16 2001-05-25 Hormos Medical Corporation Triphenylalkene derivatives and their use as selective estrogen receptor modulators
WO2002066415A2 (en) * 2001-02-20 2002-08-29 The Provost, Fellows And Scholars Of The College Of The Holy And Undivided Trinity Of Queen Elizabeth Near Dublin Non-steroidal modulators of estrogen receptors
WO2005033056A2 (en) * 2003-10-08 2005-04-14 Smithkline Beecham Corporation Triphenylethylene compounds as selective estrogen receptor modulators
WO2007062148A2 (en) * 2005-11-22 2007-05-31 Smithkline Beecham Corporation Chemical compounds
WO2007062190A2 (en) * 2005-11-22 2007-05-31 Smithkline Beecham Corporation Chemical compounds
WO2007062145A2 (en) * 2005-11-22 2007-05-31 Smithkline Beecham Corporation Chemical compounds
WO2007062151A2 (en) * 2005-11-22 2007-05-31 Smithkline Beecham Corporation Chemical compounds

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See also references of WO2013097773A1 *

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