CN102250042A - 用于治疗血管舒缩症状的选择性雌激素受体调节剂 - Google Patents

用于治疗血管舒缩症状的选择性雌激素受体调节剂 Download PDF

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Publication number
CN102250042A
CN102250042A CN2011101337521A CN201110133752A CN102250042A CN 102250042 A CN102250042 A CN 102250042A CN 2011101337521 A CN2011101337521 A CN 2011101337521A CN 201110133752 A CN201110133752 A CN 201110133752A CN 102250042 A CN102250042 A CN 102250042A
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CN
China
Prior art keywords
phenyl
base
naphthalene
fluoro
add
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Pending
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CN2011101337521A
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English (en)
Chinese (zh)
Inventor
R·D·达利
J·A·道奇
S·A·弗兰克
R·J·欣克林
T·A·谢坡德
O·B·华莱士
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Eli Lilly and Co
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Eli Lilly and Co
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Application filed by Eli Lilly and Co filed Critical Eli Lilly and Co
Publication of CN102250042A publication Critical patent/CN102250042A/zh
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/092Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings with aromatic radicals attached to the chain
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/08Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms
    • C07D295/084Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/088Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly bound oxygen or sulfur atoms with the ring nitrogen atoms and the oxygen or sulfur atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00Drugs for disorders of the endocrine system
    • A61P5/24Drugs for disorders of the endocrine system of the sex hormones
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04Ortho- or peri-condensed ring systems
    • C07D221/18Ring systems of four or more rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D311/00Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/78Ring systems having three or more relevant rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D335/00Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/04Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Reproductive Health (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Pyrane Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
CN2011101337521A 2004-01-22 2005-01-18 用于治疗血管舒缩症状的选择性雌激素受体调节剂 Pending CN102250042A (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US53844204P 2004-01-22 2004-01-22
US53834204P 2004-01-22 2004-01-22
US60/538,442 2004-01-22
US60/538,342 2004-01-22

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
CN2005800029140A Division CN1910167B (zh) 2004-01-22 2005-01-18 用于治疗血管舒缩症状的选择性雌激素受体调节剂

Publications (1)

Publication Number Publication Date
CN102250042A true CN102250042A (zh) 2011-11-23

Family

ID=34830456

Family Applications (1)

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CN2011101337521A Pending CN102250042A (zh) 2004-01-22 2005-01-18 用于治疗血管舒缩症状的选择性雌激素受体调节剂

Country Status (20)

Country Link
US (2) US20090023917A1 (https=)
EP (1) EP1709021B1 (https=)
JP (1) JP4909086B2 (https=)
KR (2) KR100849559B1 (https=)
CN (1) CN102250042A (https=)
AT (1) ATE476428T1 (https=)
AU (1) AU2005207821B2 (https=)
BR (1) BRPI0506721A (https=)
CA (1) CA2551956C (https=)
CR (1) CR8517A (https=)
DE (1) DE602005022673D1 (https=)
EA (2) EA012262B1 (https=)
EC (1) ECSP066711A (https=)
ES (1) ES2347973T3 (https=)
IL (1) IL176738A0 (https=)
MA (1) MA28436B1 (https=)
NO (1) NO20063760L (https=)
SG (1) SG149867A1 (https=)
UA (1) UA85862C2 (https=)
WO (1) WO2005073204A1 (https=)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108675999A (zh) * 2018-05-09 2018-10-19 浙江农林大学暨阳学院 一种醋酸铜催化制备8-(9-亚砜基-10-二氢菲)喹啉的方法
TWI702219B (zh) * 2018-07-12 2020-08-21 美商美國禮來大藥廠 選擇性雌激素受體降解劑

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WO2008002490A2 (en) 2006-06-23 2008-01-03 Radius Health, Inc. Treatment of vasomotor symptoms with selective estrogen receptor modulators
US10144736B2 (en) * 2006-07-20 2018-12-04 Gilead Sciences, Inc. Substituted pteridines useful for the treatment and prevention of viral infections
WO2008009078A2 (en) 2006-07-20 2008-01-24 Gilead Sciences, Inc. 4,6-dl- and 2,4,6-trisubstituted quinazoline derivatives useful for treating viral infections
CA2738878C (en) * 2008-09-29 2013-08-13 Eli Lilly And Company Selective estrogen receptor modulator for the treatment of osteoarthritis
US20100087402A1 (en) * 2008-09-29 2010-04-08 Vivus, Inc. Methods and compositions for the treatment of estrogen-dependent hyperproliferative uterine disorders
US20100317635A1 (en) 2009-06-16 2010-12-16 Endorecherche, Inc. Treatment of hot flushes, vasomotor symptoms, and night sweats with sex steroid precursors in combination with selective estrogen receptor modulators
HUE030072T2 (en) 2010-05-12 2017-04-28 Radius Health Inc Therapeutic prescriptions
US9133182B2 (en) 2010-09-28 2015-09-15 Radius Health, Inc. Selective androgen receptor modulators
FR3014437B1 (fr) * 2013-12-05 2016-12-23 Servier Lab Nouveau procede de synthese de l'agomelatine
FR3014434B1 (fr) * 2013-12-05 2015-12-25 Servier Lab Nouveau procede de synthese du 7-methoxy-naphtalene-1-carbaldehyde et application a la synthese de l'agomelatine
US9421264B2 (en) 2014-03-28 2016-08-23 Duke University Method of treating cancer using selective estrogen receptor modulators
ES3055185T3 (en) 2014-03-28 2026-02-10 Univ Duke Treatment of an estrogen receptor positive breast cancer using a selective estrogen receptor modulator
US9670205B2 (en) 2015-03-04 2017-06-06 Gilead Sciences, Inc. Toll like receptor modulator compounds
MX389702B (es) 2016-06-22 2025-03-20 Ellipses Pharma Ltd Compuestos para usarse en el tratamiento de cancer de mama que expresa el receptor de androgenos (ar+).
WO2018045150A1 (en) 2016-09-02 2018-03-08 Gilead Sciences, Inc. 4,6-diamino-pyrido[3,2-d]pyrimidine derivaties as toll like receptor modulators
AU2017318601B2 (en) 2016-09-02 2020-09-03 Gilead Sciences, Inc. Toll like receptor modulator compounds
JP7481115B2 (ja) 2017-01-05 2024-05-10 ラジウス ファーマシューティカルズ,インコーポレイテッド Rad1901-2hclの多形性形態
MX2020013713A (es) 2018-07-04 2021-03-02 Radius Pharmaceuticals Inc Formas polimorficas de rad1901-2hcl.
CN112424205B (zh) * 2018-07-12 2023-10-31 伊莱利利公司 选择性的雌激素受体降解剂
EP3924328A1 (en) 2019-02-12 2021-12-22 Radius Pharmaceuticals, Inc. Processes and compounds
TWI751516B (zh) 2019-04-17 2022-01-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TW202212339A (zh) 2019-04-17 2022-04-01 美商基利科學股份有限公司 類鐸受體調節劑之固體形式
TWI879779B (zh) 2019-06-28 2025-04-11 美商基利科學股份有限公司 類鐸受體調節劑化合物的製備方法
TWI894443B (zh) 2021-03-16 2025-08-21 美商美國禮來大藥廠 選擇性雌激素受體降解劑
CA3243621A1 (en) 2022-02-01 2023-08-10 Eli Lilly And Company METHODS FOR PREPARING SELECTIVE ESTROGEN RECEPTOR DEGRADING AGENTS

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5998401A (en) * 1995-02-28 1999-12-07 Eli Lilly And Company Naphthyl compounds, intermediates, compositions, and methods
US5726186A (en) * 1995-09-08 1998-03-10 Eli Lilly And Company Pentacyclic compounds, intermediates, processes, compositions, and methods
ID19392A (id) * 1996-08-29 1998-07-09 Lilly Co Eli Senyawa naftil dan bahan pertengahan serta komposisi dan metode penggunaan
CA2213810C (en) * 1996-08-29 2006-06-06 Lewis Dale Pennington Benzo¬b|thiophene compounds, intermediates, processes, compositions and methods
US5916916A (en) * 1996-10-10 1999-06-29 Eli Lilly And Company 1-aryloxy-2-arylnaphthyl compounds, intermediates, compositions, and methods
CA2217810A1 (en) * 1996-10-10 1998-04-10 Eli Lilly And Company 2-aryl-3-aminoaryloxynaphthyl compounds, intermediates, compositions and methods
CA2298651A1 (en) * 1997-08-07 1999-02-18 Jeffrey Alan Dodge 1-¬4-(substituted alkoxy)benzyl|naphthalene compounds having estrogen inhibitory activity
EA008024B1 (ru) * 2002-07-22 2007-02-27 Эли Лилли Энд Компани Селективные модуляторы эстрогенных рецепторов, содержащие фенилсульфонильную группу

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN108675999A (zh) * 2018-05-09 2018-10-19 浙江农林大学暨阳学院 一种醋酸铜催化制备8-(9-亚砜基-10-二氢菲)喹啉的方法
CN108675999B (zh) * 2018-05-09 2021-03-16 浙江农林大学暨阳学院 一种醋酸铜催化制备8-(9-亚砜基-10-二氢菲)喹啉类化合物的方法
TWI702219B (zh) * 2018-07-12 2020-08-21 美商美國禮來大藥廠 選擇性雌激素受體降解劑
CN112638916A (zh) * 2018-07-12 2021-04-09 伊莱利利公司 选择性雌激素受体降解剂
CN112638916B (zh) * 2018-07-12 2023-09-12 伊莱利利公司 选择性雌激素受体降解剂
CN117379428A (zh) * 2018-07-12 2024-01-12 伊莱利利公司 选择性雌激素受体降解剂

Also Published As

Publication number Publication date
US20090023917A1 (en) 2009-01-22
KR101008804B1 (ko) 2011-01-14
CR8517A (es) 2006-12-01
EA012262B1 (ru) 2009-08-28
KR20060129277A (ko) 2006-12-15
KR100849559B1 (ko) 2008-07-31
US20110281847A1 (en) 2011-11-17
US8217032B2 (en) 2012-07-10
MA28436B1 (fr) 2007-02-01
BRPI0506721A (pt) 2007-05-02
CA2551956C (en) 2013-05-07
EA016613B1 (ru) 2012-06-29
ECSP066711A (es) 2006-10-31
SG149867A1 (en) 2009-02-27
AU2005207821A1 (en) 2005-08-11
EA200900586A1 (ru) 2009-08-28
AU2005207821B2 (en) 2011-02-10
KR20080016755A (ko) 2008-02-21
NO20063760L (no) 2006-10-16
CA2551956A1 (en) 2005-08-11
ATE476428T1 (de) 2010-08-15
WO2005073204A1 (en) 2005-08-11
DE602005022673D1 (de) 2010-09-16
UA85862C2 (uk) 2009-03-10
JP4909086B2 (ja) 2012-04-04
JP2007519721A (ja) 2007-07-19
ES2347973T3 (es) 2010-11-26
IL176738A0 (en) 2006-10-31
EP1709021B1 (en) 2010-08-04
EA200601353A1 (ru) 2007-02-27
EP1709021A1 (en) 2006-10-11

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Application publication date: 20111123