PE20040678A1 - Moduladores de los receptores selectivos de estrogenos - Google Patents

Moduladores de los receptores selectivos de estrogenos

Info

Publication number
PE20040678A1
PE20040678A1 PE2003000717A PE2003000717A PE20040678A1 PE 20040678 A1 PE20040678 A1 PE 20040678A1 PE 2003000717 A PE2003000717 A PE 2003000717A PE 2003000717 A PE2003000717 A PE 2003000717A PE 20040678 A1 PE20040678 A1 PE 20040678A1
Authority
PE
Peru
Prior art keywords
selective estrogen
modulators
estrogen receptors
leiomyomata
useful
Prior art date
Application number
PE2003000717A
Other languages
English (en)
Spanish (es)
Inventor
Kin Chiu Fong
Conrad Wilson Hummel
Robert Dean Dally
Scott Alan Jones
Timothy Alan Shepherd
George Sal Lewis
Owen Brendan Wallace
Scott Alan Frank
Jeffrey Alan Dodge
Original Assignee
Lilly Co Eli
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
Application filed by Lilly Co Eli filed Critical Lilly Co Eli
Publication of PE20040678A1 publication Critical patent/PE20040678A1/es

Links

Classifications

    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Hydrogenated Pyridines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Steroid Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
PE2003000717A 2002-07-22 2003-07-18 Moduladores de los receptores selectivos de estrogenos PE20040678A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US39786902P 2002-07-22 2002-07-22
US45023303P 2003-02-25 2003-02-25

Publications (1)

Publication Number Publication Date
PE20040678A1 true PE20040678A1 (es) 2004-10-06

Family

ID=30773044

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2003000717A PE20040678A1 (es) 2002-07-22 2003-07-18 Moduladores de los receptores selectivos de estrogenos

Country Status (24)

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

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1530470B9 (en) * 2002-07-22 2010-04-07 Eli Lilly And Company Selective estrogen receptor modulators containing a phenylsulfonyl group
MXPA05009098A (es) * 2003-02-25 2005-11-17 Lilly Co Eli Clorhidrato de 1- (4-(2 -piperidiniletoxifenoxi) -2-(4-metansulfonilfenil) -6-hidroxinaftaleno cristalino no solvatado.
NZ541126A (en) * 2003-02-25 2008-07-31 Lilly Co Eli Crystalline non-solvated 1-(4-(2-piperidinylethoxy)phenoxy)-2-(4-methanesulfonylphenyl)-6-hydroxynaphthalene hydrochloride
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
US20070066595A1 (en) * 2004-01-22 2007-03-22 Dodge Jeffrey A Selective estrogen receptor modulators
SG149867A1 (en) 2004-01-22 2009-02-27 Lilly Co Eli Selective estrogen receptor modulators for the treatment of vasomotor symptoms
EP1713770A1 (en) * 2004-01-29 2006-10-25 Eli Lilly And Company Selective estrogen receptor modulators
KR20070026841A (ko) * 2004-06-22 2007-03-08 스미스클라인 비참 코포레이션 화합물
CA2617146A1 (en) * 2005-07-29 2007-02-08 Eli Lilly And Company Crystalline non-solvated methanesulfonic acid salt of 1-(4-(2-piperidinylethoxy)phenoxy)-2-(3-hydroxyphenyl)-6-hydroxynaphthalene
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
CA2754685A1 (en) 2009-03-11 2010-09-16 Pfizer Inc. Substituted indazole amides
KR20140089402A (ko) 2010-06-16 2014-07-14 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
SI2958907T1 (en) 2013-02-19 2018-05-31 Novartis Ag Benzothiophene derivatives and their compositions as selective estrogen receptor antagonists
BR112021017646A2 (pt) 2019-03-08 2021-11-16 Syngenta Crop Protection Ag Compostos de azol-amida ativos em termos pesticidas
US20220183294A1 (en) 2019-03-20 2022-06-16 Syngenta Crop Protection Ag Pesticidally active azole amide compounds
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
UY38623A (es) 2019-03-29 2020-10-30 Syngenta Crop Protection Ag Compuestos de diazina-amida activos como pesticidas
JOP20210272A1 (ar) 2019-04-05 2023-01-30 Syngenta Crop Protection Ag مركبات دايازين - أميد نشطة بشكل مبيد للآفات
JP2022545266A (ja) 2019-08-23 2022-10-26 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ピラジン-アミド化合物
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
BR112022017093A2 (pt) 2020-02-27 2023-02-14 Syngenta Crop Protection Ag Compostos de diazina-bisamida ativos em termos pesticidas
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
WO2022258481A1 (en) 2021-06-09 2022-12-15 Syngenta Crop Protection Ag Pesticidally active diazine-amide compounds
US20240208950A1 (en) * 2021-07-07 2024-06-27 South Dakota Board Of Regents Compositions and methods for treatment of cervical and ovarian cancer
EP4577532A1 (en) 2022-08-25 2025-07-02 Sanofi Novel substituted benzothiophene-6-carboxylic acid derivatives, processes for their preparation and therapeutic uses thereof

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US4418068A (en) * 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes
AU665690B2 (en) 1992-05-08 1996-01-11 Otsuka Pharmaceutical Factory, Inc. Indole derivative
US6756388B1 (en) 1993-10-12 2004-06-29 Pfizer Inc. Benzothiophenes and related compounds as estrogen agonists
US5484798A (en) * 1994-09-20 1996-01-16 Eli Lilly And Company Benzothiopene compounds, compositions, and method of inhibiting restenosis
US7501441B1 (en) 1994-09-20 2009-03-10 Eli Lilly And Company Naphthyl compounds, intermediates, processes, compositions, and methods
US5552412A (en) 1995-01-09 1996-09-03 Pfizer Inc 5-substitued-6-cyclic-5,6,7,8-tetrahydronaphthalen2-ol compounds which are useful for treating osteoporosis
US5998401A (en) * 1995-02-28 1999-12-07 Eli Lilly And Company Naphthyl compounds, intermediates, compositions, and methods
PT729956E (pt) 1995-02-28 2002-03-28 Lilly Co Eli Compostos intermediarios formulacoes e metodos de benzotiofeno
US5599822A (en) 1995-06-06 1997-02-04 Eli Lilly And Company Methods for minimizing bone loss
ATE284690T1 (de) * 1995-10-31 2005-01-15 Lilly Co Eli Antithrombotische diamine
CA2246721A1 (en) * 1996-02-22 1997-08-28 George Joseph Cullinan Benzothiophenes, formulations containing same, and methods
ES2162198T3 (es) 1996-04-19 2001-12-16 American Home Prod Agentes estrogenos.
CA2214070C (en) 1996-08-29 2006-03-14 Eli Lilly And Company Dihydronaphthalene and naphthalene compounds, intermediates, formulations, 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
CA2213814A1 (en) 1996-08-29 1998-02-28 Henry Uhlman Bryant Naphthalene compounds, intermediates, formulations, and methods
CA2217810A1 (en) * 1996-10-10 1998-04-10 Eli Lilly And Company 2-aryl-3-aminoaryloxynaphthyl compounds, intermediates, compositions and methods
CA2218756A1 (en) 1996-10-25 1998-04-25 Kristin Sue Marron Substituted benzo¢b!thiophene compounds having activity as selective estrogen receptor modulators
EP1530470B9 (en) * 2002-07-22 2010-04-07 Eli Lilly And Company Selective estrogen receptor modulators containing a phenylsulfonyl group

Also Published As

Publication number Publication date
US20060183736A1 (en) 2006-08-17
CO5680445A2 (es) 2006-09-29
CN1668303A (zh) 2005-09-14
AU2003253129A1 (en) 2004-02-09
US20080214612A1 (en) 2008-09-04
ATE433322T1 (de) 2009-06-15
EP1530470B1 (en) 2009-06-10
ES2326593T3 (es) 2009-10-15
US7399867B2 (en) 2008-07-15
DE60327931D1 (de) 2009-07-23
BR0312675A (pt) 2005-05-03
US7585977B2 (en) 2009-09-08
CN1668303B (zh) 2010-10-27
JP2005538089A (ja) 2005-12-15
NZ537138A (en) 2007-11-30
MY141879A (en) 2010-07-16
IL165745A0 (en) 2006-01-15
JP5220800B2 (ja) 2013-06-26
TWI314860B (en) 2009-09-21
CA2490580C (en) 2012-12-11
HRP20041233A2 (en) 2005-02-28
JP2010195820A (ja) 2010-09-09
AU2003253129B2 (en) 2008-12-11
CA2490580A1 (en) 2004-01-29
EP1530470B9 (en) 2010-04-07
EA008024B1 (ru) 2007-02-27
NO20050832L (no) 2005-02-16
PL374845A1 (en) 2005-11-14
MXPA05000898A (es) 2005-05-16
EP1530470A1 (en) 2005-05-18
JP4656939B2 (ja) 2011-03-23
CR7657A (es) 2005-07-13
HK1078003A1 (en) 2006-03-03
EA200500248A1 (ru) 2005-06-30
TW200414901A (en) 2004-08-16
ECSP055549A (es) 2005-03-10
WO2004009086A1 (en) 2004-01-29

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