PE20070170A1 - BENZOFURANONE DERIVATIVES AS NON-STEROID MODULATORS OF PROGESTERONE RECEPTORS - Google Patents

BENZOFURANONE DERIVATIVES AS NON-STEROID MODULATORS OF PROGESTERONE RECEPTORS

Info

Publication number
PE20070170A1
PE20070170A1 PE2006000732A PE2006000732A PE20070170A1 PE 20070170 A1 PE20070170 A1 PE 20070170A1 PE 2006000732 A PE2006000732 A PE 2006000732A PE 2006000732 A PE2006000732 A PE 2006000732A PE 20070170 A1 PE20070170 A1 PE 20070170A1
Authority
PE
Peru
Prior art keywords
phenyl
alkyl
horror
ethinyl
rac
Prior art date
Application number
PE2006000732A
Other languages
Spanish (es)
Inventor
Ulrich Bothe
Ulrike Fuhrmann
Norbert Schmees
Wolfgang Schwede
Anja Schmidt
Carsten Moller
Original Assignee
Schering Ag
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 Schering Ag filed Critical Schering Ag
Publication of PE20070170A1 publication Critical patent/PE20070170A1/en

Links

Classifications

    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • 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
    • A61P15/04—Drugs for genital or sexual disorders; Contraceptives for inducing labour or abortion; Uterotonics
    • 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
    • A61P15/08—Drugs for genital or sexual disorders; Contraceptives for gonadal disorders or for enhancing fertility, e.g. inducers of ovulation or of spermatogenesis
    • 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
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans 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
    • C07D307/83—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Pregnancy & Childbirth (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Steroid Compounds (AREA)
  • Furan Compounds (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE BENZOFURANONA DE FORMULA (I) DONDE R1 Y R2 SON INDEPENDIENTEMENTE H, ALQUILO(C1-C5) LINEAL Y/O RAMIFICADO, O FORMAN JUNTO AL C DE LA CADENA UN ANILLO DE 3 A 7 MIEMBROS; R3 ES C C-Ra; DONDE Ra ES H, ALQUILO(C1-C8), ALQUENILO(C2-C8), CICLOALQUILO(C3-C10), ARILO O HETEROARILO, ENTRE OTROS OPCIONALMENTE SUSTITUIDOS; A ES ANILLO AROMATICO CARBOCICLICO O HETEROCICLICO MONO O BICICLICO, TAL COMO FENILO O NAFTILO; B ES CARBONILO O CH2; R4a Y R4b SON INDEPENDIENTEMENTE H, ALQUILO(C1-C4), ALQUENILO(C2-C4), ENTRE OTROS. SON PREFERIDOS: RAC-5-{2-ETINIL-2-HIDROXI-3-[1-(2-FLUORO-5-TRIFLUOROMETILFENIL)-CICLOPROPIL}-PROPIONILAMINO}FTALIDA, RAC-5-{2-HIDROXI-3-[1-FENIL-CICLOPROPIL]-2-(FENIL-ETINIL)PROPIONILAMINO}-FTALIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO DE PREPARACION. ESTOS COMPUESTOS SON MODULADORES NO ESTEROIDEOS DEL RECEPTOR DE PROGESTERONA PR-B Y SON UTILES PARA EL TRATAMIENTO Y PREVENCION DE ENFERMEDADES GINECOLOGICAS COMO ENDOMETRIOSIS, LEIOMIOMAS DE UTERO, DISMENORREA, PREVENCION DE TUMORES DEPENDIENTES DE HORMONAS Y TERAPIA DE REEMPLAZO HORMONALIT REFERS TO COMPOUNDS DERIVED FROM BENZOFURANONE OF FORMULA (I) WHERE R1 AND R2 ARE INDEPENDENTLY H, LINEAR AND / OR BRANCHED ALKYL (C1-C5), OR FORM, TOGETHER TO THE C OF THE CHAIN, A RING OF 3 TO 7 MEMBERS; R3 IS C C-Ra; WHERE Ra IS H, ALKYL (C1-C8), ALKENYL (C2-C8), CYCLOALKYL (C3-C10), ARYL OR HETEROARYL, AMONG OTHERS OPTIONALLY SUBSTITUTED; A IS A CARBOYCLIC OR HETEROCICLIC, MONO OR BICYCLIC AROMATIC RING, SUCH AS PHENYL OR NAPHTHYLUS; B IS CARBONYL OR CH2; R4a AND R4b ARE INDEPENDENTLY H, ALKYL (C1-C4), ALKENYL (C2-C4), AMONG OTHERS. PREFERRED: RAC-5- {2-ETHINYL-2-HYDROXY-3- [1- (2-FLUORO-5-TRIFLUOROMETHYLPHENYL) -CYCLOPROPYL} -PROPIONYLAMINO} PHTHALIDE, RAC-5- {2-HYDROXY-3- [ 1-PHENYL-CYCLOPROPYL] -2- (PHENYL-ETHINYL) PROPIONYLAMINE} -FTALIDE, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION AND A PREPARATION PROCEDURE. THESE COMPOUNDS ARE NON-STEROID MODULATORS OF THE PR-B PROGESTERONE RECEPTOR AND ARE USEFUL FOR THE TREATMENT AND PREVENTION OF GYNECOLOGICAL DISEASES SUCH AS ENDOMETRIOSIS, LEIOMYOMAS OF THE UTERUS, DYSMENORRHEA, PREVENTION OF HORROR AND DEPENDENT HORROR TUMORS.

PE2006000732A 2005-06-24 2006-06-26 BENZOFURANONE DERIVATIVES AS NON-STEROID MODULATORS OF PROGESTERONE RECEPTORS PE20070170A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102005030294A DE102005030294A1 (en) 2005-06-24 2005-06-24 Nonsteroidal progesterone receptor modulators

Publications (1)

Publication Number Publication Date
PE20070170A1 true PE20070170A1 (en) 2007-03-02

Family

ID=36716643

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006000732A PE20070170A1 (en) 2005-06-24 2006-06-26 BENZOFURANONE DERIVATIVES AS NON-STEROID MODULATORS OF PROGESTERONE RECEPTORS

Country Status (22)

Country Link
EP (1) EP1899315A1 (en)
JP (1) JP2008543911A (en)
KR (1) KR20080018275A (en)
CN (1) CN101248056A (en)
AR (1) AR057409A1 (en)
AU (1) AU2006261049A1 (en)
BR (1) BRPI0612305A2 (en)
CA (1) CA2611900A1 (en)
CR (1) CR9595A (en)
DE (1) DE102005030294A1 (en)
DO (1) DOP2006000150A (en)
EA (1) EA200702604A1 (en)
EC (1) ECSP078043A (en)
GT (1) GT200600272A (en)
IL (1) IL188022A0 (en)
MX (1) MX2008000070A (en)
NO (1) NO20080441L (en)
PE (1) PE20070170A1 (en)
TW (1) TW200738665A (en)
UY (1) UY29626A1 (en)
WO (1) WO2006136462A1 (en)
ZA (1) ZA200800689B (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY30805A1 (en) * 2006-12-21 2008-07-31 Bayer Schering Pharma Ag NON-STEROID MODULATORS OF PROGESTERONE RECEPTORS
DE102007032800A1 (en) * 2007-07-10 2009-01-15 Bayer Schering Pharma Aktiengesellschaft Nonsteroidal progesterone receptor modulators
DE102007058747A1 (en) * 2007-12-05 2009-06-10 Bayer Schering Pharma Aktiengesellschaft Nonsteroidal progesterone receptor modulators
TWI477276B (en) * 2008-04-28 2015-03-21 Repros Therapeutics Inc Antiprogestin dosing regimens
US10328022B2 (en) 2012-05-31 2019-06-25 Repros Therapeutics Inc. Formulations and methods for vaginal delivery of antiprogestins
WO2014070517A1 (en) 2012-11-02 2014-05-08 Repros Therapeutics Inc. Methods and compositions for treating progesterone-dependent conditions

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19723722A1 (en) * 1997-05-30 1998-12-10 Schering Ag Nonsteroidal progestogens
CN1353717A (en) * 1999-05-04 2002-06-12 莱加制药公司 Tetracyclic progesterone receptor modulator compounds and methods
US6358948B1 (en) * 1999-05-04 2002-03-19 American Home Products Corporation Quinazolinone and benzoxazine derivatives as progesterone receptor modulators
AU2003202216A1 (en) * 2002-01-14 2003-07-30 Boehringer Ingelheim Pharmaceuticals, Inc. Glucocorticoid mimetics, methods of making them, pharmaceutical formulations containing them and uses thereof
EP1482925B1 (en) * 2002-03-11 2007-01-17 Schering AG 5-(2-hydroxy-3-'1-(3-trifluoromethylphenyl)-cyclopropl]-propionylamino)-phtalide and related compounds with progesterone receptor modulating activity for use in fertility control and hormone replacement therapy
DE10346939A1 (en) * 2003-10-06 2005-05-19 Schering Ag New arylalkanol derivatives used for treating e.g. respiratory diseases, joint diseases, vascular inflammations, skin disorders, kidney and liver diseases and neurological diseases

Also Published As

Publication number Publication date
AU2006261049A1 (en) 2006-12-28
EP1899315A1 (en) 2008-03-19
GT200600272A (en) 2007-08-20
DE102005030294A1 (en) 2007-01-04
BRPI0612305A2 (en) 2010-11-03
DOP2006000150A (en) 2006-12-31
ECSP078043A (en) 2008-01-23
NO20080441L (en) 2008-03-07
AR057409A1 (en) 2007-12-05
UY29626A1 (en) 2007-01-31
JP2008543911A (en) 2008-12-04
MX2008000070A (en) 2008-03-19
KR20080018275A (en) 2008-02-27
TW200738665A (en) 2007-10-16
ZA200800689B (en) 2009-07-29
IL188022A0 (en) 2008-03-20
CN101248056A (en) 2008-08-20
WO2006136462A1 (en) 2006-12-28
CA2611900A1 (en) 2006-12-28
CR9595A (en) 2008-05-05
EA200702604A1 (en) 2008-06-30

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