CN1668303B - 含苯磺酰基的选择性雌激素受体调节剂 - Google Patents

含苯磺酰基的选择性雌激素受体调节剂 Download PDF

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Publication number
CN1668303B
CN1668303B CN038172011A CN03817201A CN1668303B CN 1668303 B CN1668303 B CN 1668303B CN 038172011 A CN038172011 A CN 038172011A CN 03817201 A CN03817201 A CN 03817201A CN 1668303 B CN1668303 B CN 1668303B
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mmol
added
compound
phenyl
dichloromethane
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Expired - Fee Related
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CN038172011A
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Chinese (zh)
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CN1668303A (zh
Inventor
R·D·达利
J·A·多奇
S·A·弗兰克
S·A·琼斯
T·A·谢菲尔德
O·B·华莱士
K·C·冯
C·W·胡梅尔
G·S·路易斯
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Eli Lilly and Co
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Eli Lilly and Co
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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
    • C07D295/088Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/08Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • 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
    • A61P5/30Oestrogens
    • 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
    • A61P5/32Antioestrogens
    • 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
    • C07D295/12Heterocyclic 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 or doubly bound nitrogen atoms
    • C07D295/125Heterocyclic 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 or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13Heterocyclic 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 or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/54Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/56Radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the hetero ring
    • C07D333/64Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/72Benzo[c]thiophenes; Hydrogenated benzo[c]thiophenes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Hydrogenated Pyridines (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CN038172011A 2002-07-22 2003-07-16 含苯磺酰基的选择性雌激素受体调节剂 Expired - Fee Related CN1668303B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US39786902P 2002-07-22 2002-07-22
US60/397,869 2002-07-22
US45023303P 2003-02-25 2003-02-25
US60/450,233 2003-02-25
PCT/IB2003/003349 WO2004009086A1 (en) 2002-07-22 2003-07-16 Selective estrogen receptor modulators containing a phenylsulfonyl group

Publications (2)

Publication Number Publication Date
CN1668303A CN1668303A (zh) 2005-09-14
CN1668303B true CN1668303B (zh) 2010-10-27

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US (2) US7399867B2 (https=)
EP (1) EP1530470B9 (https=)
JP (2) JP4656939B2 (https=)
CN (1) CN1668303B (https=)
AT (1) ATE433322T1 (https=)
AU (1) AU2003253129B2 (https=)
BR (1) BR0312675A (https=)
CA (1) CA2490580C (https=)
CO (1) CO5680445A2 (https=)
CR (1) CR7657A (https=)
DE (1) DE60327931D1 (https=)
EA (1) EA008024B1 (https=)
EC (1) ECSP055549A (https=)
ES (1) ES2326593T3 (https=)
HR (1) HRP20041233A2 (https=)
IL (1) IL165745A0 (https=)
MX (1) MXPA05000898A (https=)
MY (1) MY141879A (https=)
NO (1) NO20050832L (https=)
NZ (1) NZ537138A (https=)
PE (1) PE20040678A1 (https=)
PL (1) PL374845A1 (https=)
TW (1) TWI314860B (https=)
WO (1) WO2004009086A1 (https=)

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CN100348192C (zh) * 2003-02-25 2007-11-14 伊莱利利公司 晶状的非溶剂化1-(4-(2-哌啶基乙氧基)苯氧基)-2-(4-甲磺酰基苯基)-6-羟基萘盐酸化物
EP1709021B1 (en) * 2004-01-22 2010-08-04 Eli Lilly And Company Selective estrogen receptor modulators for the treatment of vasomotor symptoms
ATE448215T1 (de) * 2004-01-22 2009-11-15 Lilly Co Eli Selektive östrogen-rezeptor-modulatoren
CN1910167B (zh) * 2004-01-22 2011-08-10 伊莱利利公司 用于治疗血管舒缩症状的选择性雌激素受体调节剂
EP1713770A1 (en) * 2004-01-29 2006-10-25 Eli Lilly And Company Selective estrogen receptor modulators
CA2571309A1 (en) * 2004-06-22 2006-01-05 Smithkline Beecham Corporation Chemical compounds
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EA020742B1 (ru) * 2008-09-29 2015-01-30 Эли Лилли Энд Компани Селективный модулятор рецепторов эстрогена
DE102008057230A1 (de) * 2008-11-11 2010-05-12 Bayer Schering Pharma Aktiengesellschaft Synergistische pharmazeutische Kombination mit einem Estrogenrezeptorantagonisten und einem Progestin
US20110319379A1 (en) 2009-03-11 2011-12-29 Corbett Jeffrey W Substituted Indazole Amides And Their Use As Glucokinase Activators
KR20200144591A (ko) 2010-06-16 2020-12-29 앙도르쉐르슈 인코포레이티드 에스트로겐-관련 질병의 치료 또는 예방 방법
JP6292744B2 (ja) * 2012-09-19 2018-03-14 富士カプセル株式会社 医薬品組成物
BR112015018882B1 (pt) 2013-02-19 2021-09-14 Novartis Ag Derivados de benzotiofeno e composições dos mesmos como degradadores de receptor de estrogênio seletivo
WO2020182649A1 (en) 2019-03-08 2020-09-17 Syngenta Crop Protection Ag Pesticidally active azole-amide compounds
BR112021018501A2 (pt) 2019-03-20 2021-11-30 Syngenta Crop Protection Ag Compostos de azolamida ativos em termos pesticidas
CN113597426A (zh) 2019-03-22 2021-11-02 先正达农作物保护股份公司 N-[1-(5-溴-2-嘧啶-2-基-1,2,4-三唑-3-基)乙基]-2-环丙基-6-(三氟甲基)吡啶-4-甲酰胺衍生物及相关的化合物作为杀昆虫剂
TWI853009B (zh) 2019-03-29 2024-08-21 瑞士商先正達農作物保護公司 殺有害生物活性之二-醯胺化合物
JP7611848B2 (ja) 2019-04-05 2025-01-10 シンジェンタ クロップ プロテクション アクチェンゲゼルシャフト 殺有害生物的に活性なジアジン-アミド化合物
BR112022003375A2 (pt) 2019-08-23 2022-05-17 Syngenta Crop Protection Ag Compostos de pirazina-amida pesticidamente ativos
CN110526881B (zh) * 2019-08-27 2020-09-22 河南省锐达医药科技有限公司 一种萘胺类化合物及其生物学可接受的盐,其制备方法和应用
JP2023515979A (ja) 2020-02-27 2023-04-17 シンジェンタ クロップ プロテクション アクチェンゲゼルシャフト 殺有害生物的に活性なジアジン-ビスアミド化合物
WO2022237904A1 (zh) * 2021-05-14 2022-11-17 江苏亚虹医药科技股份有限公司 一种含萘环的化合物、含其的药物组合物及其应用
JP2024524883A (ja) 2021-06-09 2024-07-09 シンジェンタ クロップ プロテクション アクチェンゲゼルシャフト 殺有害生物的に活性なジアジン-アミド化合物
US20240208950A1 (en) * 2021-07-07 2024-06-27 South Dakota Board Of Regents Compositions and methods for treatment of cervical and ovarian cancer
CN119768396A (zh) 2022-08-25 2025-04-04 赛诺菲 新颖的取代的苯并噻吩-6-羧酸衍生物、其制备方法及其治疗用途

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JP2010195820A (ja) 2010-09-09
EP1530470B9 (en) 2010-04-07
CA2490580C (en) 2012-12-11
MY141879A (en) 2010-07-16
TW200414901A (en) 2004-08-16
US20080214612A1 (en) 2008-09-04
EP1530470A1 (en) 2005-05-18
ES2326593T3 (es) 2009-10-15
AU2003253129A1 (en) 2004-02-09
DE60327931D1 (de) 2009-07-23
JP2005538089A (ja) 2005-12-15
BR0312675A (pt) 2005-05-03
PL374845A1 (en) 2005-11-14
CR7657A (es) 2005-07-13
CO5680445A2 (es) 2006-09-29
PE20040678A1 (es) 2004-10-06
NZ537138A (en) 2007-11-30
EA200500248A1 (ru) 2005-06-30
WO2004009086A1 (en) 2004-01-29
CA2490580A1 (en) 2004-01-29
AU2003253129B2 (en) 2008-12-11
US7585977B2 (en) 2009-09-08
EA008024B1 (ru) 2007-02-27
EP1530470B1 (en) 2009-06-10
US7399867B2 (en) 2008-07-15
ECSP055549A (es) 2005-03-10
MXPA05000898A (es) 2005-05-16
IL165745A0 (en) 2006-01-15
US20060183736A1 (en) 2006-08-17
JP4656939B2 (ja) 2011-03-23
TWI314860B (en) 2009-09-21
JP5220800B2 (ja) 2013-06-26
CN1668303A (zh) 2005-09-14
HRP20041233A2 (en) 2005-02-28
ATE433322T1 (de) 2009-06-15
NO20050832L (no) 2005-02-16
HK1078003A1 (en) 2006-03-03

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