ES2183288T3 - Compuestos de indeno con actividad como moduladores selectivos de receptores de estrogenos. - Google Patents

Compuestos de indeno con actividad como moduladores selectivos de receptores de estrogenos.

Info

Publication number
ES2183288T3
ES2183288T3 ES98303132T ES98303132T ES2183288T3 ES 2183288 T3 ES2183288 T3 ES 2183288T3 ES 98303132 T ES98303132 T ES 98303132T ES 98303132 T ES98303132 T ES 98303132T ES 2183288 T3 ES2183288 T3 ES 2183288T3
Authority
ES
Spain
Prior art keywords
activity
indene
compounds
pyrrolidinyl
possess
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.)
Expired - Lifetime
Application number
ES98303132T
Other languages
English (en)
Inventor
Henry Uhlman Bryant
Charles David Jones
Pamela Ann Pennington
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.)
Eli Lilly and Co
Original Assignee
Eli Lilly and Co
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 Eli Lilly and Co filed Critical Eli Lilly and Co
Application granted granted Critical
Publication of ES2183288T3 publication Critical patent/ES2183288T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • 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
    • A61P5/30—Oestrogens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C43/00—Ethers; Compounds having groups, groups or groups
    • C07C43/02—Ethers
    • C07C43/20—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring
    • C07C43/23—Ethers having an ether-oxygen atom bound to a carbon atom of a six-membered aromatic ring containing hydroxy or O-metal groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D339/00—Heterocyclic compounds containing rings having two sulfur atoms as the only ring hetero atoms
    • C07D339/08—Six-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/08—One of the condensed rings being a six-membered aromatic ring the other ring being five-membered, e.g. indane

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Obesity (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)

Abstract

LA PRESENTE INVENCION PROPORCIONA UNA CLASE DE COMPUESTOS DE INDENO SUSTITUIDOS Y SUS SALES FARMACEUTICAMENTE ACEPTABLES, QUE POSEEN ACTIVIDAD MODULADORA SELECTIVA DE LOS RECEPTORES DE ESTROGENO (SERM) Y SON UTILES POR TANTO PARA EL TRATAMIENTO DE LA OSTEOPOROSIS Y LA ENFERMEDAD CARDIOVASCULAR, ESPECIALMENTE LA HIPERLIPIDEMIA EN MUJERES. DICHOS COMPUESTOS POSEEN LA ESTRUCTURA: DONDE R 1 ES HIDROGENO, HIDROXILO, ALCOXI, FENILC ARBONILOXI, ALQUILCARBONILOXI O ALQUILSULFONILOXI; R 2 ES HIDROGENO, HIDROXILO, HALO, ALCOXI, FENILCARBONILOXI, ALQUILCARBONILOXI O ALQUILSULFONILOXI; R 3 ES 1 - PIPERIDINILO, 1 PIRROLIDINILO, METIL - 1 - PIRROLIDINILO, DIMETIL - 1 PIRROLIDINILO, 4 - MORFOLINO, DIMETILAMINO, DIETILAMINO, DIISOPROPILAMINO O 1 - HEXAMETILENIMINO; Y N ES 1, 2 O 3. EL ENLACE REPRESENTADO POR LA LINEA DISCONTINUA ENTRE LOS ATOMOS DE CARBONO SITUADOS EN LAS POSICIONES 1 Y 2 DEL NUCLEO DE INDENO REPRESENTA UN ENLACE DOBLE OPCIONAL, CON LA CONDICION DE QUE CUANDO EL ENLACE DOBLE ESTA AUSENTE,EL GRUPO HIDROXILO ENTRE PARENTESIS SITUADO EN POSICION 1 ESTA PRESENTE Y VICEVERSA. CIERTOS PRECURSORES 2, 3 - DIHIDRO - 1H - INDENO DE LOS COMPUESTOS DE INDENO DESCRITOS POSEEN TAMBIEN ACTIVIDAD SERM Y SON UTILES PARA LOS MISMOS FINES.
ES98303132T 1997-04-25 1998-04-23 Compuestos de indeno con actividad como moduladores selectivos de receptores de estrogenos. Expired - Lifetime ES2183288T3 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US4492397P 1997-04-25 1997-04-25

Publications (1)

Publication Number Publication Date
ES2183288T3 true ES2183288T3 (es) 2003-03-16

Family

ID=21935066

Family Applications (1)

Application Number Title Priority Date Filing Date
ES98303132T Expired - Lifetime ES2183288T3 (es) 1997-04-25 1998-04-23 Compuestos de indeno con actividad como moduladores selectivos de receptores de estrogenos.

Country Status (9)

Country Link
US (1) US5994370A (es)
EP (1) EP0873992B1 (es)
JP (1) JP2002510289A (es)
AT (1) ATE224883T1 (es)
AU (1) AU7467398A (es)
CA (1) CA2287244A1 (es)
DE (1) DE69808169T2 (es)
ES (1) ES2183288T3 (es)
WO (1) WO1998048806A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002016316A1 (en) * 2000-08-23 2002-02-28 Akzo Nobel N.V. 10-ARYL-11-HBENZO [b]FLUORENE DERIVATIVES AND ANALOGS FOR MEDICINAL USE
DE60112624T2 (de) * 2001-01-04 2006-06-08 Karo Bio Ab Östrogenrezeptor-Liganden und Verfahren
WO2002056903A2 (en) * 2001-01-17 2002-07-25 Praecis Pharmaceuticals Inc. Methods for treating hormone associated conditions using a combination of lhrh antagonists and specific estrogen receptor modulators
TW200304371A (en) 2002-02-22 2003-10-01 Akzo Nobel Nv Substituted 10-ary1-11H-benzo [b] fluorenes and 7-ary1-5, 6-dihydro-benz [a] anthracenes for selective effects on estrogen receptors
MXPA05003054A (es) * 2002-09-20 2005-05-27 Pfizer Prod Inc Ligandos de amida y sulfonamida para el receptor de estrogenos.
KR100595963B1 (ko) 2004-04-13 2006-07-05 한국화학연구원 인덴 유도체 및 이의 제조방법
US8853423B2 (en) 2010-06-17 2014-10-07 Seragon Pharmaceuticals, Inc. Indane estrogen receptor modulators and uses thereof

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3274213A (en) * 1961-09-05 1966-09-20 Upjohn Co Alkoxy-substituted 2-phenyl-1-(tertiary-aminoalkoxy)phenyl-3, 4-dihydronaphthalenes
DE1300575B (de) * 1965-05-21 1969-08-07 Bristol Myers Co Benzo[b]thiophene
US3394125A (en) * 1965-10-23 1968-07-23 Bristol Myers Co 2-phenyl-3-tertiary-aminoalkoxy phenyl-and corresponding tertiaryaminoalkyl thio benzfurans substituted in the benzo nucleus with an alkoxy or tertiaryamino alkoxy or alkylthio group
US3483293A (en) * 1967-12-15 1969-12-09 Upjohn Co Method for controlling birds and rodents
US4133814A (en) * 1975-10-28 1979-01-09 Eli Lilly And Company 2-Phenyl-3-aroylbenzothiophenes useful as antifertility agents
US4230862A (en) * 1975-10-28 1980-10-28 Eli Lilly And Company Antifertility compounds
US4418068A (en) * 1981-04-03 1983-11-29 Eli Lilly And Company Antiestrogenic and antiandrugenic benzothiophenes
US4380635A (en) * 1981-04-03 1983-04-19 Eli Lilly And Company Synthesis of acylated benzothiophenes
US4358593A (en) * 1981-04-03 1982-11-09 Eli Lilly And Company Process for preparing 3-(4-aminoethoxybenzoyl)benzo[b]thiophenes
GB2097788B (en) * 1981-04-03 1985-04-24 Lilly Co Eli Benzothiophene compounds and process for preparing them
US4729999A (en) * 1984-10-12 1988-03-08 Bcm Technologies Antiestrogen therapy for symptoms of estrogen deficiency
AU621811B2 (en) * 1987-09-25 1992-03-26 Ciba-Geigy Ag Diacyl derivatives of 4-(trialkylbenzyl)-piperazinyl compounds
US5395842A (en) * 1988-10-31 1995-03-07 Endorecherche Inc. Anti-estrogenic compounds and compositions
DE4117512A1 (de) * 1991-05-25 1992-11-26 Schering Ag 2-phenylbenzo(b)furane und -thiophene, verfahren zu deren herstellung und diese enthaltende pharmazeutische praeparate
US5147880A (en) * 1991-07-22 1992-09-15 Eli Lilly And Company Benzo[a]fluorene compounds
JP3157882B2 (ja) * 1991-11-15 2001-04-16 帝国臓器製薬株式会社 新規なベンゾチオフエン誘導体
US6756388B1 (en) * 1993-10-12 2004-06-29 Pfizer Inc. Benzothiophenes and related compounds as estrogen agonists
US5591753A (en) * 1994-01-28 1997-01-07 Eli Lilly And Company Combination treatment for osteoporosis
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
US6391892B1 (en) * 1995-03-10 2002-05-21 Eli Lilly And Company Naphthyl pharmaceutical compounds
US6451817B1 (en) * 1995-03-10 2002-09-17 Eli Lilly And Company Alpha-substituted-1-benzyl-napthyls
US5811421A (en) * 1995-07-31 1998-09-22 Eli Lilly And Company Naphthyl and dihydronaphthyl intermediates, compounds, compositions, and methods
CA2213814A1 (en) * 1996-08-29 1998-02-28 Henry Uhlman Bryant Naphthalene compounds, intermediates, formulations, 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

Also Published As

Publication number Publication date
JP2002510289A (ja) 2002-04-02
US5994370A (en) 1999-11-30
WO1998048806A1 (en) 1998-11-05
EP0873992B1 (en) 2002-09-25
EP0873992A1 (en) 1998-10-28
CA2287244A1 (en) 1998-11-05
ATE224883T1 (de) 2002-10-15
AU7467398A (en) 1998-11-24
DE69808169T2 (de) 2003-05-22
DE69808169D1 (de) 2002-10-31

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