AR022797A1 - BENZOIL INDOLES N-SUBSTITUTED AS ESTROGEN AGENTS - Google Patents

BENZOIL INDOLES N-SUBSTITUTED AS ESTROGEN AGENTS

Info

Publication number
AR022797A1
AR022797A1 ARP000100898A ARP000100898A AR022797A1 AR 022797 A1 AR022797 A1 AR 022797A1 AR P000100898 A ARP000100898 A AR P000100898A AR P000100898 A ARP000100898 A AR P000100898A AR 022797 A1 AR022797 A1 AR 022797A1
Authority
AR
Argentina
Prior art keywords
alkyl
ethers
branched
straight
estrogen
Prior art date
Application number
ARP000100898A
Other languages
Spanish (es)
Original Assignee
Wyeth Corp
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 Wyeth Corp filed Critical Wyeth Corp
Publication of AR022797A1 publication Critical patent/AR022797A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/12—Radicals substituted by oxygen atoms
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system

Abstract

La presente provee compuestos de la formula (1) donde: R1, R2 y R3 se seleccionan independientemente de hidrogeno, alquilo C1-6, alcoxi C1-6, -CF3, -NO2,ciano, alquilo C1-6 (de cadena recta o ramificada), trifluorometilo, -OH o ésteres C1-12 (de cadena recta o ramificada) o sus alquil éteres C1-12 (de cadenarecta o ramificada o cíclica), halogenos, o éteres halogenados C1-6; preferentemente éteres halogenados de C1-3, incluyendo a trifluorometil éter ytriclorometil éter; R4 y R5 se seleccionan independientemente de H o bencilo, el grupo bencilo está opcionalmente sustituido por alquilo C1-6, alcoxi C1-6,-CF3, o halogeno; X es H, alquilo C1-6, o CF3; Z es O o S; n es 2 o 3; e Y se selecciona de: a) una porcion de la formula (2) donde R es alquilo inferiorC1-6; o b) una porcion seleccionada del grupo formado por las formulas (3), (4), (5) o (6); o su sal farmacéuticamente aceptable, así como también lasformulaciones farmacéuticas y métodos para tratar o prevenir estados o síndromes de enfermedades que están causadas o asociadas con una deficiencia deestrogeno o un exceso de estrogeno que utiliza a estos compuestos.This provides compounds of the formula (1) where: R1, R2 and R3 are independently selected from hydrogen, C1-6 alkyl, C1-6 alkoxy, -CF3, -NO2, cyano, C1-6 alkyl (straight chain or branched), trifluoromethyl, -OH or C1-12 esters (straight or branched chain) or their C1-12 alkyl ethers (straight or branched or cyclic chain), halogens, or halogenated C1-6 ethers; preferably C1-3 halogenated ethers, including trifluoromethyl ether andtrichloromethyl ether; R4 and R5 are independently selected from H or benzyl, the benzyl group is optionally substituted by C1-6 alkyl, C1-6 alkoxy, -CF3, or halogen; X is H, C1-6 alkyl, or CF3; Z is O or S; n is 2 or 3; and Y is selected from: a) a portion of the formula (2) where R is C1-6 lower alkyl; or b) a portion selected from the group consisting of formulas (3), (4), (5) or (6); or its pharmaceutically acceptable salt, as well as pharmaceutical formulations and methods to treat or prevent conditions or syndromes of diseases that are caused or associated with an estrogen deficiency or an excess of estrogen that uses these compounds.

ARP000100898A 1999-03-04 2000-03-01 BENZOIL INDOLES N-SUBSTITUTED AS ESTROGEN AGENTS AR022797A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26241399A 1999-03-04 1999-03-04

Publications (1)

Publication Number Publication Date
AR022797A1 true AR022797A1 (en) 2002-09-04

Family

ID=22997395

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP000100898A AR022797A1 (en) 1999-03-04 2000-03-01 BENZOIL INDOLES N-SUBSTITUTED AS ESTROGEN AGENTS

Country Status (8)

Country Link
EP (1) EP1159268A1 (en)
JP (1) JP2002538141A (en)
CN (1) CN1342144A (en)
AR (1) AR022797A1 (en)
AU (1) AU3859400A (en)
CA (1) CA2364914A1 (en)
MX (1) MXPA01008911A (en)
WO (1) WO2000051983A1 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5998402A (en) 1996-04-19 1999-12-07 American Home Products Corporation 2-phenyl-1-[4-(2-aminoethoxy)-benzyl]-indoles as estrogenic agents
US7528165B2 (en) 2001-12-13 2009-05-05 National Health Research Institutes Indole compounds
TWI317634B (en) 2001-12-13 2009-12-01 Nat Health Research Institutes Aroyl indoles compounds
US7632955B2 (en) 2001-12-13 2009-12-15 National Health Research Institutes Indole compounds
MXPA05003054A (en) * 2002-09-20 2005-05-27 Pfizer Prod Inc Amide and sulfonamide ligands for the estrogen receptor.
CN100506795C (en) * 2003-06-18 2009-07-01 中国科学院上海药物研究所 Indene ketone diindyl class compound, preparation method and medical use thereof
US7250440B2 (en) * 2003-08-12 2007-07-31 Wyeth (Hydroxyphenyl)-1H-indole-3-carbaldehyde oxime derivatives as estrogenic agents
US7456289B2 (en) 2004-12-31 2008-11-25 National Health Research Institutes Anti-tumor compounds
DK2276732T3 (en) 2008-04-16 2015-08-17 Karobio Ab Novel østrogenreceptorligander

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0639567A1 (en) * 1992-05-08 1995-02-22 Otsuka Pharmaceutical Factory, Inc. Indole derivative
ES2162198T3 (en) * 1996-04-19 2001-12-16 American Home Prod STROGEN AGENTS.

Also Published As

Publication number Publication date
WO2000051983A1 (en) 2000-09-08
AU3859400A (en) 2000-09-21
CN1342144A (en) 2002-03-27
MXPA01008911A (en) 2002-10-23
EP1159268A1 (en) 2001-12-05
CA2364914A1 (en) 2000-09-08
JP2002538141A (en) 2002-11-12

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Legal Events

Date Code Title Description
FA Abandonment or withdrawal