BRPI0508256A - hidróxi-6-fenilfenantridinas heterociclila-substituìdas e o uso da mesma como inibidores de pde4 - Google Patents

hidróxi-6-fenilfenantridinas heterociclila-substituìdas e o uso da mesma como inibidores de pde4

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Publication number
BRPI0508256A
BRPI0508256A BRPI0508256-0A BRPI0508256A BRPI0508256A BR PI0508256 A BRPI0508256 A BR PI0508256A BR PI0508256 A BRPI0508256 A BR PI0508256A BR PI0508256 A BRPI0508256 A BR PI0508256A
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Brazil
Prior art keywords
alkyl
alkoxy
hydrogen
substituted
hydroxy
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BRPI0508256-0A
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English (en)
Inventor
Ulrich Kautz
Beate Schmidt
Dieter Flockerzi
Armin Hatzelmann
Zitt Christof
Johannes Barsig
Degenhard Marx
Hans-Peter Kley
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Altana Pharma Ag
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Application filed by Altana Pharma Ag filed Critical Altana Pharma Ag
Publication of BRPI0508256A publication Critical patent/BRPI0508256A/pt

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    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • C07D221/10—Aza-phenanthrenes
    • C07D221/12—Phenanthridines
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D221/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02—Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04—Ortho- or peri-condensed ring systems
    • C07D221/06—Ring systems of three rings
    • 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
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/473—Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
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    • A—HUMAN NECESSITIES
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/10—Heterocyclic 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 carbon chain containing aromatic rings
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings

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  • Health & Medical Sciences (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Ophthalmology & Optometry (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
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  • Orthopedic Medicine & Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

"HIDRóXI-6 FENILFENANTRIDINAS HETEROCICLILA-SUBSTITUìDAS E O USO DA MESMA COMO INIBIDORES DE PDE4" A presente invenção refere-se a Compostos de fórmula (I) em que r1 é idrixila,1-4C-alcóxi,3-7Ccicloalcóxi, 3-7C cicloalquimetóxi, 2,2-difluoroetóxi, ou 1-4C-alcóxi completamenteou predominantemente flúor-substituido, R2 é hidroxila, 1-4C-alcóxi, 37C-cicloalcóxi, 3-7C- cicloalquilmetóxi, 2,2-dufluoroetóxi, ou 1-4C-alcóxi completemente ou predominantemente flúor-substituído, ou em R1 e R2 juntos são um grupo 1-2C alquilenodióxi, R3 é hidrogênio ou 1-4C alquila,R31 é hidrogênio ou 1-4C alquila, ou uma primeira modalidade (modalidade a ) de acordo com a presente inevneção, R4 é -O-R41, em que R41 é hidrogênio, 1-4C-alquila, 1-4C- alcóxi-14C-alquila, hidróxi-2-C-alquila, 1-7C-alquilcarbonila, ou 1-4C-alquil completamente ou predominantemente flúor-substituído, R5 é hidrogênio ou 1-4C-alquila, ou em uma segunda modalidade (modalidade b) de acordo com a presente invenção, R4 é hidrogênio ou 1-4C-alquila, e R5 é -O-R51, em que R51 é hidrogênio, 1-4C alquila, 1-4C-alcóxi-1-4C-alquila, hidróxi-2-4C-alquila, 1-7C alquicarbonila, ou 1-4C alquila completamente ou prediminantemente flúor-substituído, R6 é hidrogênio, halogênio, 1-4C-alquil ou 1-4C-alcóxi, R7 é Het1, Het2,Hart, Het3, ou Har2,em que.
BRPI0508256-0A 2004-03-03 2005-03-03 hidróxi-6-fenilfenantridinas heterociclila-substituìdas e o uso da mesma como inibidores de pde4 BRPI0508256A (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP04005005 2004-03-03
EP04106372 2004-12-07
PCT/EP2005/050946 WO2005090311A1 (en) 2004-03-03 2005-03-03 Novel heterocyclyl-substituted hydroxy-6-phenylphenanthridines and their use as pde4 inhibitors

Publications (1)

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BRPI0508256A true BRPI0508256A (pt) 2007-07-31

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ID=34961674

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BRPI0508256-0A BRPI0508256A (pt) 2004-03-03 2005-03-03 hidróxi-6-fenilfenantridinas heterociclila-substituìdas e o uso da mesma como inibidores de pde4

Country Status (13)

Country Link
US (1) US20070191413A1 (pt)
EP (1) EP1812400A1 (pt)
JP (1) JP2007526284A (pt)
KR (1) KR20060130684A (pt)
AR (1) AR049419A1 (pt)
AU (1) AU2005223370A1 (pt)
BR (1) BRPI0508256A (pt)
CA (1) CA2557730A1 (pt)
IL (1) IL177301A0 (pt)
NO (1) NO20064220L (pt)
NZ (1) NZ549109A (pt)
TW (1) TW200540157A (pt)
WO (1) WO2005090311A1 (pt)

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EP1539164B1 (en) * 2002-08-29 2006-12-20 ALTANA Pharma AG 2-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
WO2004019945A1 (en) 2002-08-29 2004-03-11 Altana Pharma Ag 3-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
ES2400823T3 (es) 2004-02-18 2013-04-12 Takeda Gmbh Nuevas hidroxi-6-fenilfenantridinas sustituidas con guanidinilo como inhibidores eficaces de fosfodiesterasa (PDE) 4
SG182194A1 (en) 2004-03-03 2012-07-30 Nycomed Gmbh Novel hydroxy-6-heteroarylphenanthridines and their use as pde4 inhibitors
CA2558391A1 (en) * 2004-03-10 2005-09-22 Altana Pharma Ag Novel amido-substituted hydroxy-6-phenylphenanthridines and their use as pde4 inhibitors
JP5478828B2 (ja) 2005-03-02 2014-04-23 タケダ ゲゼルシャフト ミット ベシュレンクテル ハフツング ６−ヘテロシクリル置換されたヘキサヒドロフェナントリジン誘導体の新規の塩
EP2207540B1 (en) 2007-10-04 2014-02-26 F. Hoffmann-La Roche AG Cyclopropyl aryl amide derivatives and uses thereof

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Also Published As

Publication number Publication date
EP1812400A1 (en) 2007-08-01
WO2005090311A1 (en) 2005-09-29
NZ549109A (en) 2010-05-28
NO20064220L (no) 2006-09-18
TW200540157A (en) 2005-12-16
CA2557730A1 (en) 2005-09-29
AU2005223370A1 (en) 2005-09-29
AR049419A1 (es) 2006-08-02
WO2005090311A8 (en) 2006-10-26
US20070191413A1 (en) 2007-08-16
IL177301A0 (en) 2006-12-10
KR20060130684A (ko) 2006-12-19
JP2007526284A (ja) 2007-09-13

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