KR100849559B1 - 혈관운동 증상의 치료를 위한 선택적 에스트로겐 수용체조절제 - Google Patents

혈관운동 증상의 치료를 위한 선택적 에스트로겐 수용체조절제 Download PDF

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KR100849559B1
KR100849559B1 KR1020067014630A KR20067014630A KR100849559B1 KR 100849559 B1 KR100849559 B1 KR 100849559B1 KR 1020067014630 A KR1020067014630 A KR 1020067014630A KR 20067014630 A KR20067014630 A KR 20067014630A KR 100849559 B1 KR100849559 B1 KR 100849559B1
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mmol
phenyl
added
naphthalen
ethoxy
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KR20060129277A (ko
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로버트 딘 댈리
제프리 알란 닷지
스코트 알란 프랭크
로날드 제이 힌클린
티모시 알란 셰퍼드
오웬 브렌던 월레스
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일라이 릴리 앤드 캄파니
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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
    • C07D295/08—Heterocyclic 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
    • C07D295/084—Heterocyclic 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
    • C07D295/092—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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
    • C07D295/08—Heterocyclic 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
    • C07D295/084—Heterocyclic 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
    • C07D295/088—Heterocyclic 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic 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
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/18—Ring systems of four or more rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic 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
    • C07D311/78—Ring systems having three or more relevant rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D335/00—Heterocyclic compounds containing six-membered rings having one sulfur atom as the only ring hetero atom
    • C07D335/04—Heterocyclic 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)
KR1020067014630A 2004-01-22 2005-01-18 혈관운동 증상의 치료를 위한 선택적 에스트로겐 수용체조절제 Expired - Fee Related KR100849559B1 (ko)

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 Child Applications (1)

Application Number Title Priority Date Filing Date
KR1020087003065A Division KR101008804B1 (ko) 2004-01-22 2005-01-18 혈관운동 증상의 치료를 위한 선택적 에스트로겐 수용체조절제

Publications (2)

Publication Number Publication Date
KR20060129277A KR20060129277A (ko) 2006-12-15
KR100849559B1 true KR100849559B1 (ko) 2008-07-31

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Application Number Title Priority Date Filing Date
KR1020067014630A Expired - Fee Related KR100849559B1 (ko) 2004-01-22 2005-01-18 혈관운동 증상의 치료를 위한 선택적 에스트로겐 수용체조절제
KR1020087003065A Expired - Fee Related KR101008804B1 (ko) 2004-01-22 2005-01-18 혈관운동 증상의 치료를 위한 선택적 에스트로겐 수용체조절제

Family Applications After (1)

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KR1020087003065A Expired - Fee Related KR101008804B1 (ko) 2004-01-22 2005-01-18 혈관운동 증상의 치료를 위한 선택적 에스트로겐 수용체조절제

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=)

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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
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
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
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
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

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EP0761669A2 (en) * 1995-09-08 1997-03-12 Eli Lilly And Company Pentacyclic compounds, intermediates, processes, compositions, and methods
EP0826679A2 (en) * 1996-08-29 1998-03-04 Eli Lilly And Company Naphthyl compounds, intermediates, compositions, and method of use
EP0835868A1 (en) * 1996-10-10 1998-04-15 Eli Lilly And Company 2-Aryl-3-aminoaryloxynaphthyl compounds, intermediates, compositions and methods
EP0895989A1 (en) * 1997-08-07 1999-02-10 Eli Lilly And Company 1-[4-(Substituted alkoxy)benzyl] naphthalene compounds having estrogen inhibitory activity

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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
EA008024B1 (ru) * 2002-07-22 2007-02-27 Эли Лилли Энд Компани Селективные модуляторы эстрогенных рецепторов, содержащие фенилсульфонильную группу

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EP0761669A2 (en) * 1995-09-08 1997-03-12 Eli Lilly And Company Pentacyclic compounds, intermediates, processes, compositions, and methods
EP0826679A2 (en) * 1996-08-29 1998-03-04 Eli Lilly And Company Naphthyl compounds, intermediates, compositions, and method of use
EP0835868A1 (en) * 1996-10-10 1998-04-15 Eli Lilly And Company 2-Aryl-3-aminoaryloxynaphthyl compounds, intermediates, compositions and methods
EP0895989A1 (en) * 1997-08-07 1999-02-10 Eli Lilly And Company 1-[4-(Substituted alkoxy)benzyl] naphthalene compounds having estrogen inhibitory activity

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
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
CN102250042A (zh) 2011-11-23
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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