AR049419A1 - Hidroxi-6-fenilfenantridinas sustituidas con heterociclilo - Google Patents

Hidroxi-6-fenilfenantridinas sustituidas con heterociclilo

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Publication number
AR049419A1
AR049419A1 ARP050100781A ARP050100781A AR049419A1 AR 049419 A1 AR049419 A1 AR 049419A1 AR P050100781 A ARP050100781 A AR P050100781A AR P050100781 A ARP050100781 A AR P050100781A AR 049419 A1 AR049419 A1 AR 049419A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
completely
substituted
heterocyclic ring
Prior art date
Application number
ARP050100781A
Other languages
English (en)
Inventor
Ulrich Kautz
Beate Schmidt
Dieter Flockerzi
Armin Hatzelmann
Christof Zitt
Johannes Barsig
Degenhard Marx
Hans-Peter Kley
Original Assignee
Altana Pharma 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 Altana Pharma Ag filed Critical Altana Pharma Ag
Publication of AR049419A1 publication Critical patent/AR049419A1/es

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    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D221/10—Aza-phenanthrenes
    • C07D221/12—Phenanthridines
    • C—CHEMISTRY; METALLURGY
    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • 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
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/08—Bronchodilators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • 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
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • 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
    • A61P17/04—Antipruritics
    • 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
    • A61P17/06—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
    • 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
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/16—Otologicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • 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)
  • Transplantation (AREA)
  • 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

Reivindicacion 1: Compuestos de la formula (1) en la cual: R1 es hidroxilo, alcoxi C1-4, cicloalcoxi C3-7, cicloalquil C3-7-metoxi, 2,2-difluoroetoxi, o alcoxi C1-4 completamente o predominantemente sustituido con F; R2 es hidroxilo, alcoxi C1-4, cicloalcoxi C3-7, cicloalquil C3-7-metoxi, 2,2-difluoroetoxi, o alcoxi C1-4 completamente o predominantemente sustituido con F; o en la cual R1 y R2 juntos son un grupo alquilendioxi C1-2; R3 es H o alquilo C1-4; R31 es H o alquilo C1-4; y en una primera realizacion (realizacion a) de acuerdo con la presente, R4 es -O-R41, en donde R41 es H, alquilo C1-4, alcoxi C1-4-alquilo C1-4, hidroxialquilo C2-4, alquil C1-7-carbonilo o alquilo C1-4 completamente o predominantemente sustituido por F, y R5 es H o alquilo C1-4; o, en una segunda realizacion (realizacion b) de acuerdo con la presente, R4 es H o alquilo C1-4 y R5 es -O-R51, en donde R51 es H, alquilo C1-4, alcoxi C1-4-alquilo C1-4, hidroxialquilo C2-4, alquil C1-7-carbonilo o alquilo C1-4 completamente o predominantemente sustituido con F; R6 es H, halogeno, alquilo C1-4 o alcoxi C1-4; R7 es Het1, Het2, Har1, Het3 o Har2, en donde Het1 está sustituido opcionalmente con R71 y es un radical de anillo heterocíclico completamente saturado, de 3 a 7 miembros, monocíclico, que comprende uno a tres heteroátomos seleccionados independientemente del grupo que consiste de N, O y S, en donde R71 es alquilo C1-4, alcoxi C1-4 o alquilo C1-4 completamente o parcialmente sustituido con F; Het2 está opcionalmente sustituido con R72 y es un radical de anillo heterocíclico, saturado o insaturado, de 5 a 7 miembros, monocíclico, que comprende un átomo de N y opcionalmente uno o dos heteroátomos adicionales seleccionados independientemente del grupo que consiste de N, O y S y a cuyo anillo están ligados uno o dos sustituyentes oxo, en donde R72 es alquilo C1-4, alcoxi C1-4 o alquilo C1-4 completamente o parcialmente sustituido con F; Har1 está opcionalmente sustituido con R73 y es un radical de anillo heterocíclico completamente insaturado, de 5 miembros, monocíclico, que comprende uno a cuatro heteroátomos seleccionados independientemente del grupo que consiste de N, O y S, en donde R73 es alquilo C1- 4, alcoxi C1-4 o alquilo C1-4 completamente o parcialmente sustituido con F; Het3 está opcionalmente sustituido con R74 y es un radical de anillo heterocíclico parcialmente insaturado, de 5 o 6 miembros, monocíclico, que comprende un átomo de N y opcionalmente un heteroátomo adicional seleccionado del grupo que consiste de N, O y S, en donde R74 es alquilo C1-4, alcoxi C1-4 o alquilo C1-4 completamente o parcialmente sustituido con F; Har2 está opcionalmente sustituido con R75 y/o R76 y significa un radical de anillo heterocíclico completamente insaturado, de 6 miembros, monocíclico, que comprende uno a tres átomos de N, en donde R75 es alquilo C1-4, alcoxi C1-4, alquiltio C1-4, halogeno, hidroxilo, amino, mono- o dialquil C1-4- amino, o alquilo C1-4 completamente o parcialmente sustituido con F; R76 es alcoxi C1-4, alquiltio C1-4, hidroxilo, amino o mono- o dialquil C1-4-amino, y las sales, los N-oxidos y las sales de los N-oxidos de estos compuestos.
ARP050100781A 2004-03-03 2005-03-02 Hidroxi-6-fenilfenantridinas sustituidas con heterociclilo AR049419A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP04005005 2004-03-03
EP04106372 2004-12-07

Publications (1)

Publication Number Publication Date
AR049419A1 true AR049419A1 (es) 2006-08-02

Family

ID=34961674

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050100781A AR049419A1 (es) 2004-03-03 2005-03-02 Hidroxi-6-fenilfenantridinas sustituidas con heterociclilo

Country Status (13)

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

Families Citing this family (7)

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Publication number Priority date Publication date Assignee Title
AU2003273805B8 (en) 2002-08-29 2010-06-17 Takeda Gmbh 3-hydroxy-6-phenylphenanthridines as PDE-4 inhibitors
DE60310576T2 (de) * 2002-08-29 2007-10-31 Altana Pharma Ag 2-hydroxy-6-phenylphenanthridine als pde-4-hemmer
CA2556086C (en) 2004-02-18 2014-04-01 Altana Pharma Ag Novel guanidinyl-substituted hydroxy-6-phenylphenenthridines as effective phosphodiesterase (pde) 4 inhibitors
ES2505473T3 (es) 2004-03-03 2014-10-10 Takeda Gmbh Nuevas hidroxi-6-heteroarilfenantridinas y su uso como inhibidores de la PDE4
KR20060130697A (ko) * 2004-03-10 2006-12-19 알타나 파마 아게 신규한 아미도-치환 히드록시-6-페닐페난트리딘 및 ｐｄｅ4억제제로서의 이의 용도
US7718668B2 (en) 2005-03-02 2010-05-18 Nycomed Gmbh Salts of 6-heterocycle substituted hexahydrophenanthridine derivatives
WO2009043784A1 (en) 2007-10-04 2009-04-09 F. Hoffmann-La Roche Ag Cyclopropyl aryl amide derivatives and uses thereof

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Also Published As

Publication number Publication date
JP2007526284A (ja) 2007-09-13
US20070191413A1 (en) 2007-08-16
NO20064220L (no) 2006-09-18
KR20060130684A (ko) 2006-12-19
BRPI0508256A (pt) 2007-07-31
WO2005090311A1 (en) 2005-09-29
TW200540157A (en) 2005-12-16
NZ549109A (en) 2010-05-28
EP1812400A1 (en) 2007-08-01
CA2557730A1 (en) 2005-09-29
AU2005223370A1 (en) 2005-09-29
WO2005090311A8 (en) 2006-10-26
IL177301A0 (en) 2006-12-10

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