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

Hidroxi-6-fenilfenantridinas sustituidas con heterociclilo

Info

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)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Cardiology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Gynecology & Obstetrics (AREA)
  • Transplantation (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Epidemiology (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)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1539164B1 (en) * 2002-08-29 2006-12-20 ALTANA Pharma AG 2-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
EP1536798B1 (en) 2002-08-29 2007-02-07 ALTANA Pharma AG 3-hydroxy-6-phenylphenanthridines as pde-4 inhibitors
CA2556086C (en) 2004-02-18 2014-04-01 Altana Pharma Ag Novel guanidinyl-substituted hydroxy-6-phenylphenenthridines as effective phosphodiesterase (pde) 4 inhibitors
CN104761545A (zh) 2004-03-03 2015-07-08 塔科达有限责任公司 新的羟基-6-杂芳基菲啶及其作为pde4抑制剂的用途
BRPI0508481A (pt) * 2004-03-10 2007-07-31 Altana Pharma Ag hidróxi-6-fenilenantridinas amido-substituìdas e seu uso como inibidores de pde4
NZ589278A (en) 2005-03-02 2012-04-27 Nycomed Gmbh Selected salts of 6-heterocyclyl substituted hexahydrophenanthridine derivatives
AU2008307195B2 (en) 2007-10-04 2012-11-22 F. Hoffmann-La Roche Ag Cyclopropyl aryl amide derivatives and uses thereof

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BR9707233A (pt) * 1996-01-31 1999-07-20 Byk Gulden Lomberg Chem Fab Fenantridinas
US6127378A (en) * 1996-03-26 2000-10-03 Byk Gulden Lomberg Chemische Fabrik Gmbh Phenanthridines substituted in the 6 position
CZ288752B6 (cs) * 1996-11-11 2001-08-15 Byk Gulden Lomberg Chemische Fabrik Gmbh Benzonaftyridinové deriváty a farmaceutický prostředek
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JP2007527899A (ja) * 2004-03-09 2007-10-04 アルタナ　ファルマ　アクチエンゲゼルシャフト 新規のイソアミド置換されたヒドロキシ−６−フェニルフェナントリジン
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BRPI0508481A (pt) * 2004-03-10 2007-07-31 Altana Pharma Ag hidróxi-6-fenilenantridinas amido-substituìdas e seu uso como inibidores de pde4
WO2005087744A1 (en) * 2004-03-10 2005-09-22 Altana Pharma Ag Novel thio-containing hydroxy-6-phenylphenanthridines and their use as pde4 inhibitors
JP2008528556A (ja) * 2005-02-01 2008-07-31 ニコメッド ゲゼルシャフト ミット ベシュレンクテル ハフツング 新規の６−ピリジルフェナントリジン
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EP1858880A1 (en) * 2005-03-09 2007-11-28 Nycomed GmbH Amido-substituted 6-phenylphenanthridines
US20070154915A1 (en) * 2005-11-04 2007-07-05 Johji Inazawa Method for detecting cancer and a method for suppressing cancer

Also Published As

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

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