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PE20070125A1 - NON-STEROID PROGESTERONE RECEPTOR MODULATORS - Google Patents

NON-STEROID PROGESTERONE RECEPTOR MODULATORS

Info

Publication number
PE20070125A1
PE20070125A1 PE2006000733A PE2006000733A PE20070125A1 PE 20070125 A1 PE20070125 A1 PE 20070125A1 PE 2006000733 A PE2006000733 A PE 2006000733A PE 2006000733 A PE2006000733 A PE 2006000733A PE 20070125 A1 PE20070125 A1 PE 20070125A1
Authority
PE
Peru
Prior art keywords
alkyl
methyl
progesterone receptor
receptor modulators
benzoxazin
Prior art date
Application number
PE2006000733A
Other languages
Spanish (es)
Inventor
Ulrich Bothe
Peter Droescher
Ulrike Fuhrmann
Alexander Hillisch
Guenter Kaufmann
Carsten Moller
Norbert Schmees
Wolfgang Schwede
Lothar Sobek
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 PE20070125A1 publication Critical patent/PE20070125A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/536Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with carbocyclic ring systems
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • A61P5/34Gestagens
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/021,2-Oxazines; Hydrogenated 1,2-oxazines

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Pregnancy & Childbirth (AREA)
  • Gynecology & Obstetrics (AREA)
  • Diabetes (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE R1 Y R2 SON CADA UNO H, ALQUILO C1-C5 LINEAL O NO LINEAL, RAMIFICADO O NO; R3 ES CC-Ra; Ra ES H, ALQUILO C1-C8, ALQUENILO C2-C8, CICLOALQUILO C3-C10, ENTRE OTROS; R4 ES H, METILO, ETILO, ALQUILO C1-C3 PARCIAL O TOTALMENTE FLUORADO; A ES ANILLO AROMATICO MONO O BICICLICO, CARBOCICLICO O HETEROCICLICO, OPCIONALMENTE MONO O POLI SUSTITUIDO CON ALQUILO C1-C8, ALQUENILO C2-C8, PERFLUOROALQUILO C1-C6, ENTRE OTROS; B ES CARBONILO, CH2. SON COMPUESTOS PREFERIDOS: (-)-6-{2-[2-(2,3-(METILENDIOXI)FENIL)-2-METILPROPIL]-2-HIDROXI-OCT-3-INAOIL}-4-METIL-2,3-BENZOXAZIN-1-ONA; 6-{2-[2-(2,3-DIHIDRO-7-BENZOFURANIL)-2-METILPROPIL]-2-HIDROXI-3-OCTINILAMINO}-4-METIL-2,3-BENZOXAZIN-1-ONA; ENTRE OTROS. REFERIDA TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON MODULADORES NO ESTEROIDES DE RECEPTOR DE PROGESTERONAIT REFERS TO A COMPOUND OF FORMULA I, WHERE R1 AND R2 ARE EACH H, C1-C5 ALKYL LINEAR OR NON-LINEAR, BRANCHED OR NOT; R3 IS CC-Ra; Ra IS H, C1-C8 ALKYL, C2-C8 ALKENYL, C3-C10 CYCLOALKYL, AMONG OTHERS; R4 IS H, METHYL, ETHYL, C1-C3 ALKYL PARTIALLY OR FULLY FLUORATED; A IS AROMATIC RING, MONO OR BICYCLIC, CARBOCYCLIC OR HETEROCICLIC, OPTIONALLY MONO OR POLY, SUBSTITUTED WITH C1-C8 ALKYL, C2-C8 ALKENYL, C1-C6 PERFLUOROALKYL, AMONG OTHERS; B IS CARBONYL, CH2. PREFERRED COMPOUNDS ARE: (-) - 6- {2- [2- (2,3- (METHYLEDIOXY) PHENYL) -2-METHYLPROPYL] -2-HYDROXY-OCT-3-INAOYL} -4-METHYL-2,3 -BENZOXAZIN-1-ONA; 6- {2- [2- (2,3-DIHYDRO-7-BENZOFURANIL) -2-METHYLPROPYL] -2-HYDROXY-3-OCTINYLAMINO} -4-METHYL-2,3-BENZOXAZIN-1-ONA; AMONG OTHERS. ALSO REFERRED TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE NON-STEROID MODULATORS OF PROGESTERONE RECEPTOR

PE2006000733A 2005-06-24 2006-06-26 NON-STEROID PROGESTERONE RECEPTOR MODULATORS PE20070125A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102005030292A DE102005030292A1 (en) 2005-06-24 2005-06-24 Nonsteroidal progesterone receptor modulators

Publications (1)

Publication Number Publication Date
PE20070125A1 true PE20070125A1 (en) 2007-02-14

Family

ID=37199176

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006000733A PE20070125A1 (en) 2005-06-24 2006-06-26 NON-STEROID PROGESTERONE RECEPTOR MODULATORS

Country Status (22)

Country Link
EP (1) EP1902049A2 (en)
JP (1) JP2008543910A (en)
KR (1) KR20080030622A (en)
CN (1) CN101248066A (en)
AR (1) AR054519A1 (en)
AU (1) AU2006261048A1 (en)
BR (1) BRPI0611903A2 (en)
CA (1) CA2611897A1 (en)
CR (1) CR9598A (en)
DE (1) DE102005030292A1 (en)
DO (1) DOP2006000148A (en)
EA (1) EA200702524A1 (en)
EC (1) ECSP078044A (en)
GT (1) GT200600271A (en)
IL (1) IL188021A0 (en)
MX (1) MX2008000072A (en)
NO (1) NO20080440L (en)
PE (1) PE20070125A1 (en)
TW (1) TW200740778A (en)
UY (1) UY29624A1 (en)
WO (1) WO2006136461A2 (en)
ZA (1) ZA200800690B (en)

Families Citing this family (4)

* 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
JP2011519916A (en) * 2008-07-02 2011-07-14 ファーマコステック カンパニー リミテッド Method for producing amide derivative

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19856475A1 (en) * 1998-11-27 2000-05-31 Schering Ag Nonsteroidal anti-inflammatories
EP1344776A1 (en) * 2002-03-11 2003-09-17 Schering Aktiengesellschaft 5- 2-hydroxy-3-[1-(3-trifluoromethylphenyl)-cyclopropyl]-propionylamino -phtalide and 6- 2-hydroxy-3-[1-(3-trifluoromethylphenyl)-cyclopropyl]-propionylamino -4-methyl-2,3-benzoxazin-1-one derivatives with progesterone receptor modulating activity for use in fertility control, hormone replacement therapy and the treatment of gynecological disorders
RS20050974A (en) * 2003-07-01 2007-09-21 Schering Aktiengesellschaft, Heterocyclically substituted pentanol derivatives,method for the production thereof,and use thereof as anti- inflammatory agents

Also Published As

Publication number Publication date
EA200702524A1 (en) 2008-06-30
IL188021A0 (en) 2008-03-20
DOP2006000148A (en) 2007-07-15
CR9598A (en) 2008-04-09
EP1902049A2 (en) 2008-03-26
UY29624A1 (en) 2007-01-31
MX2008000072A (en) 2008-03-24
KR20080030622A (en) 2008-04-04
TW200740778A (en) 2007-11-01
ECSP078044A (en) 2008-01-23
ZA200800690B (en) 2009-09-30
DE102005030292A1 (en) 2007-01-11
GT200600271A (en) 2007-02-05
BRPI0611903A2 (en) 2010-10-05
JP2008543910A (en) 2008-12-04
NO20080440L (en) 2008-03-25
CN101248066A (en) 2008-08-20
AR054519A1 (en) 2007-06-27
CA2611897A1 (en) 2006-12-28
AU2006261048A1 (en) 2006-12-28
WO2006136461A2 (en) 2006-12-28
WO2006136461A3 (en) 2007-03-15

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