BR9809703A - Acilanilidas (hetero) ciclicamente substituìdas, não esteroidais, com eficácia gestagênica e androgênica mista - Google Patents

Acilanilidas (hetero) ciclicamente substituìdas, não esteroidais, com eficácia gestagênica e androgênica mista

Info

Publication number
BR9809703A
BR9809703A BR9809703-2A BR9809703A BR9809703A BR 9809703 A BR9809703 A BR 9809703A BR 9809703 A BR9809703 A BR 9809703A BR 9809703 A BR9809703 A BR 9809703A
Authority
BR
Brazil
Prior art keywords
group
gestagenic
treatment
alkyl group
addition
Prior art date
Application number
BR9809703-2A
Other languages
English (en)
Inventor
Manfred Lahmann
Klaus Schoellkopf
Peter Strehlke
Nikolaus Heinrich
Karl-Heinrich Fritzemeier
Hans-Peter Muhn
Rolf Krattenmacher
Original Assignee
Schering Aktiengellschaft
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=7831567&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR9809703(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Aktiengellschaft filed Critical Schering Aktiengellschaft
Publication of BR9809703A publication Critical patent/BR9809703A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
    • C07D285/04—Thiadiazoles; Hydrogenated thiadiazoles not condensed with other rings
    • C07D285/10—1,2,5-Thiadiazoles; Hydrogenated 1,2,5-thiadiazoles
    • 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
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/18—Feminine contraceptives
    • 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
    • A61P5/26—Androgens
    • 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
    • A61P5/34—Gestagens
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C225/00—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
    • C07C225/22—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/32—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C07C235/38—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton containing six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/84—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/57—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and carboxyl groups, other than cyano groups, bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D237/00—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/26—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings condensed with carbocyclic rings or ring systems
    • C07D237/30—Phthalazines
    • C07D237/32—Phthalazines with oxygen atoms directly attached to carbon atoms of the nitrogen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
    • C07D249/18—Benzotriazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/02—1,2-Oxazines; Hydrogenated 1,2-oxazines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/08—1,2,5-Oxadiazoles; Hydrogenated 1,2,5-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans
    • C07D307/88—Benzo [c] furans; Hydrogenated benzo [c] furans with one oxygen atom directly attached in position 1 or 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/94—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom spiro-condensed with carbocyclic rings or ring systems, e.g. griseofulvins
    • 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
    • C07D311/76—Benzo[c]pyrans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/72—Benzo[c]thiophenes; Hydrogenated benzo[c]thiophenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Endocrinology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Reproductive Health (AREA)
  • Diabetes (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Materials For Medical Uses (AREA)
  • Steroid Compounds (AREA)

Abstract

Patente de Invenção:<B>"ACILANILIDAS (HETERO) CICLICAMENTE SUBSTITUìDAS, NãO ESTEROIDAIS, COM EFICáCIA GESTAGêNICA E ANDROGêNICA MISTA"<D>. A presente invenção descreve agentes gestagênicos não esteroidais da fórmula geral (I), na qual R^ 1^ e R^ 2^ são iguais ou diferentes e representam um átomo de hidrogênio, um grupo C~ 1~-C~ 5~ alquila ou um átomo de halogênio, além disso, em conjunto com o átomo de carbono da cadeia, representa um anel com, no total, 3-7 membros, R^ 3^ representa um grupo C~ 1~-C~ 5~- alquila ou um grupo C~ 1~-C~ 5~- alquila parcialmente ou completamente fluorado, A representa um anel aromático mono- ou bicíclico eventualmente substituído, representa um grupo éster - COOR^ 4^, representa um grupo alquenila - CR^ 5^=CR^ 6^R^ 7^, representa um grupo alquinila - C-<154>CR^ 6^R^ 7^, representa um grupo C~ 1~-C~ 5~- alquila parcialmente ou completamente fluorado; B representa um grupo carbonila ou um grupo CH~ 2~ e Ar representa adicionalmente um sistema de anel, escolhido das fórmulas parciais gerais (2-11), além disso, para o caso em que B, na fórmula geral (I), represente um grupo -CH~ 2~-, Ar adicionalmente representa um radical fenila da fórmula parcial geral (12). Os novos compostos mostram uma afinidade muito forte com relação ao receptor gestagênico. Eles podem ser utilizados isoladamente ou em combinação com estrogênios, em preparados para a contracepção. Além disso, eles podem servir para o tratamento da endometriose. Em conjunto com estrogênios, eles também podem ser utilizados em preparados para o tratamento de distúrbios ginecológicos para o tratamento de reclamações pré-menstruais e para a terapia de substituição. Com base na eficácia androgênica, eles também podem servir para o controle de fertilidade masculino, HRT masculina e terapia com hormónios e para o tratamento de quadros de doenças andrológicas.
BR9809703-2A 1997-05-30 1998-06-02 Acilanilidas (hetero) ciclicamente substituìdas, não esteroidais, com eficácia gestagênica e androgênica mista BR9809703A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19723722A DE19723722A1 (de) 1997-05-30 1997-05-30 Nichtsteroidale Gestagene
PCT/EP1998/003242 WO1998054159A1 (de) 1997-05-30 1998-06-02 Nichtsteroidale (hetero)zyklisch-substituierte acylanilide mit gemischter gestagener und androgener wirksamkeit

Publications (1)

Publication Number Publication Date
BR9809703A true BR9809703A (pt) 2000-07-11

Family

ID=7831567

Family Applications (1)

Application Number Title Priority Date Filing Date
BR9809703-2A BR9809703A (pt) 1997-05-30 1998-06-02 Acilanilidas (hetero) ciclicamente substituìdas, não esteroidais, com eficácia gestagênica e androgênica mista

Country Status (30)

Country Link
EP (1) EP0986545B1 (pt)
JP (1) JP2002502385A (pt)
KR (1) KR100536870B1 (pt)
CN (1) CN100445272C (pt)
AR (1) AR011480A1 (pt)
AT (1) ATE286035T1 (pt)
AU (1) AU747083C (pt)
BG (1) BG64212B1 (pt)
BR (1) BR9809703A (pt)
CA (1) CA2305458C (pt)
CZ (1) CZ296377B6 (pt)
DE (2) DE19723722A1 (pt)
EA (1) EA004306B1 (pt)
EE (1) EE04492B1 (pt)
ES (1) ES2234121T3 (pt)
HR (1) HRP980289B1 (pt)
HU (1) HUP0002126A3 (pt)
ID (1) ID23499A (pt)
IL (2) IL133195A0 (pt)
IS (1) IS2498B (pt)
NO (1) NO325076B1 (pt)
NZ (1) NZ501359A (pt)
PL (1) PL197887B1 (pt)
PT (1) PT986545E (pt)
SK (1) SK284943B6 (pt)
TR (1) TR199902924T2 (pt)
TW (1) TW577882B (pt)
UA (1) UA64752C2 (pt)
WO (1) WO1998054159A1 (pt)
ZA (1) ZA984655B (pt)

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CA2305458A1 (en) 1998-12-03
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HRP980289A2 (en) 1999-02-28
ATE286035T1 (de) 2005-01-15
AU747083C (en) 2004-01-29
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