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AR048001A1 - Hidroxi - 6 - fenilantridinas que contienen tio con actividad inhibitoria de pde4 y composiciones farmaceuticas que las contienen para el tratamiento de trastornos respiratorios. - Google Patents

Hidroxi - 6 - fenilantridinas que contienen tio con actividad inhibitoria de pde4 y composiciones farmaceuticas que las contienen para el tratamiento de trastornos respiratorios.

Info

Publication number
AR048001A1
AR048001A1 ARP050100916A ARP050100916A AR048001A1 AR 048001 A1 AR048001 A1 AR 048001A1 AR P050100916 A ARP050100916 A AR P050100916A AR P050100916 A ARP050100916 A AR P050100916A AR 048001 A1 AR048001 A1 AR 048001A1
Authority
AR
Argentina
Prior art keywords
alkyl
hydrogen
alkoxy
fluorine
accordance
Prior art date
Application number
ARP050100916A
Other languages
English (en)
Inventor
Ulrich Kautz
Beate Schmidt
Armin Hatzelmann
Christof Zitt
Johannes Barsig
Degenhard Marx
Hans-Peter Kley
Dieter Flockerzl
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 AR048001A1 publication Critical patent/AR048001A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic 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
    • C07D221/04Ortho- or peri-condensed ring systems
    • C07D221/06Ring systems of three rings
    • C07D221/10Aza-phenanthrenes
    • C07D221/12Phenanthridines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/02Nasal agents, e.g. decongestants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10Drugs for genital or sexual disorders; Contraceptives for impotence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/04Antipruritics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/08Antiallergic 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
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Neurology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Neurosurgery (AREA)
  • Rheumatology (AREA)
  • Biomedical Technology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Cardiology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Otolaryngology (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)

Abstract

Compuestos de formula (1), en donde R1, R2, R3, R31, R4, R5, R6 y R7 tienen los significados indicados en la que exhiben actividad inhibidora de PDE4 y son utiles en el tratamiento de trastornos respiratorios. Reivindicacion 1: Compuestos caracterizados porque responden a la formula (1), en donde: R1 es hidroxilo, C1-4-alcoxi, C3-7-cicloalcoxi, C3-7-cicloalquilmetoxi, 2,2-difluoroetoxi, o C1-4-alcoxi completamente o predominantemente sustituido por fluor; R2 es hidroxilo, C1-4- alcoxi, C3-7-cicloalcoxi, C3-7-cicloalquilmetoxi, 2,2-difluoroetoxi, o C1-4-alcoxi completamente o predominantemente sustituido por fluor; o en donde, R1 y R2 juntos son un grupo C1-2-alquilendioxi; R3 es hidrogeno o C1-4-alquilo; R31 es hidrogeno o C1-4-alquilo, ya sea, en una primera realizacion (realizacion a) de acuerdo con la presente; R4 es -O-R41, en donde, R41 es hidrogeno, C1-4-alquilo, C1-4-alcoxi-C1-4-alquilo, hidroxi-C2-4-alquilo, C1-7-alquilcarbonilo, o C1-4-alquilo completamente o predominantemente sustituido por fluor; y R5 es hidrogeno o C1-4-alquilo; o, en una segunda realizacion (realizacion b) de acuerdo con la presente; R4 es hidrogeno o C1-4-alquilo; y R5 es -O-R51, en donde, R51 es hidrogeno, C1-4-alquilo, C1-4-alcoxi- C1-4-alquilo, hidroxi-C2-4-alquilo, C1-7-alquilcarbonilo, o C1-4-alquilo completamente o predominantemente sustituido por fluor; R6 es hidrogeno, halogeno, C1-4-alquilo o C1-4-alcoxi, en un primer (aspecto 1) de acuerdo con la presente; R7 es - S(O)2N(R8)R9, en donde, R8 es hidrogeno, C1-4-alquilo, C1-4-alcoxi-C2-4-alquilo o C3-7-cicloalquilo; R9 es hidrogeno, C1-4-alquilo o C1-4-alcoxi-C2-4-alquilo, o R8 y R9 juntos e incluyendo el átomo de nitrogeno al que están unidos, forman un anillo heterociclo Het1, en donde, Het1 está opcionalmente sustituido por R81, y es un radical de anillo heterocíclico saturado de 3 a 7 miembros que corresponde el átomo de nitrogeno, al cual R8 y R9 están unidos, y opcionalmente un heteroátomo adicional seleccionado del grupo que consiste de oxígeno, nitrogeno y sulfuro, en donde, R81 es C1-4-alquilo; o, en un segundo aspecto (aspecto 2) de acuerdo con esta presente; R7 es -A-N(R10)S(O)2-R11, en donde, A es un enlace o C1-4-alquileno; R10 es hidrogeno o C1-4-alquilo; R11 es C1-4-alquilo, o fenilo R111-sustituido, en donde R111 es halogeno o C1-4-alquilo; o en un tercer aspecto (aspecto 3) de acuerdo con la presente; R7 es -S(O)nR12, en donde, n es 0, 1 o 2, R12 es C1-4-alquilo, y las sales, los N-oxidos y las sales de los N-oxidos de estos compuestos.
ARP050100916A 2004-03-10 2005-03-10 Hidroxi - 6 - fenilantridinas que contienen tio con actividad inhibitoria de pde4 y composiciones farmaceuticas que las contienen para el tratamiento de trastornos respiratorios. AR048001A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP04100988 2004-03-10
EP05100692 2005-02-01

Publications (1)

Publication Number Publication Date
AR048001A1 true AR048001A1 (es) 2006-03-15

Family

ID=34961402

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050100916A AR048001A1 (es) 2004-03-10 2005-03-10 Hidroxi - 6 - fenilantridinas que contienen tio con actividad inhibitoria de pde4 y composiciones farmaceuticas que las contienen para el tratamiento de trastornos respiratorios.

Country Status (12)

Country Link
US (1) US20080161339A1 (es)
EP (1) EP1725533A1 (es)
JP (1) JP2007527900A (es)
KR (1) KR20060124783A (es)
AR (1) AR048001A1 (es)
AU (1) AU2005221831A1 (es)
BR (1) BRPI0508473A (es)
CA (1) CA2558390A1 (es)
IL (1) IL177499A0 (es)
NO (1) NO20064416L (es)
TW (1) TW200540159A (es)
WO (1) WO2005087744A1 (es)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
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
CA2556086C (en) 2004-02-18 2014-04-01 Altana Pharma Ag Novel guanidinyl-substituted hydroxy-6-phenylphenenthridines as effective phosphodiesterase (pde) 4 inhibitors
EP1723135B1 (en) 2004-03-03 2013-06-19 Takeda GmbH Novel hydroxy-6-heroarylphenanthridines and their use as pde4 inhibitors
AR049419A1 (es) * 2004-03-03 2006-08-02 Altana Pharma Ag Hidroxi-6-fenilfenantridinas sustituidas con heterociclilo
MXPA06009892A (es) * 2004-03-10 2007-03-01 Altana Pharma Ag Nuevas hidroxi-6-fenilfenantridinas sustituidas con amido y su uso como inhibidores de la fosfodiesterasa tipo 4 (pde4).
DK1856093T3 (da) 2005-03-02 2010-03-15 Nycomed Gmbh (2R,4aR,10bR)-6-(2,6-dimethoxypyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydrophenanthridin-2-ol, HCI-salt
GB0601951D0 (en) 2006-01-31 2006-03-15 Novartis Ag Organic compounds
BRPI0718266A2 (pt) 2006-10-30 2014-01-07 Novartis Ag Compostos heterocíclicos como agentes anti-inflamatórios.
ES2460897T3 (es) 2007-10-04 2014-05-14 F. Hoffmann-La Roche Ag Derivados de ciclopropil aril amida y usos de los mismos
PT2231642E (pt) 2008-01-11 2014-03-12 Novartis Ag Pirimidinas como inibidores de quinase
US8637516B2 (en) 2010-09-09 2014-01-28 Irm Llc Compounds and compositions as TRK inhibitors
WO2012034095A1 (en) 2010-09-09 2012-03-15 Irm Llc Compounds and compositions as trk inhibitors
EA201391230A1 (ru) 2011-02-25 2014-01-30 АйАрЭм ЭлЭлСи Соединения и композиции в качестве ингибиторов trk

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CZ289340B6 (cs) * 1996-01-31 2002-01-16 Byk Gulden Lomberg Chemische Fabrik Gmbh Fenanthridinové deriváty a farmaceutický prostředek s jejich obsahem
ES2184077T3 (es) * 1996-03-26 2003-04-01 Altana Pharma Ag Nuevas fenantridinas sustituidas en la posicion 6.
US6127378A (en) * 1996-03-26 2000-10-03 Byk Gulden Lomberg Chemische Fabrik Gmbh Phenanthridines substituted in the 6 position
US6121279A (en) * 1997-07-25 2000-09-19 Byk Gulden Lomberg Chemische Fabrik Gmbh Substituted 6-phenylphenanthridines
EP0998460B1 (en) * 1997-07-25 2004-03-03 ALTANA Pharma AG Novel tetrazole derivatives
JP2002513793A (ja) * 1998-05-05 2002-05-14 ビイク グルデン ロンベルク ヒエーミツシエ フアブリーク ゲゼルシヤフト ミツト ベシユレンクテル ハフツング 新規n−オキシド
SI1147089T1 (sl) * 1999-01-15 2006-04-30 Altana Pharma Ag Fenilfenantridini z inhibirajoco aktivnostjo za PDE-IV
JP4587294B2 (ja) * 2002-08-29 2010-11-24 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 Pde4インヒビターとしての2−ヒドロキシ−6−フェニルフェナントリジン

Also Published As

Publication number Publication date
JP2007527900A (ja) 2007-10-04
US20080161339A1 (en) 2008-07-03
EP1725533A1 (en) 2006-11-29
AU2005221831A1 (en) 2005-09-22
CA2558390A1 (en) 2005-09-22
WO2005087744A1 (en) 2005-09-22
BRPI0508473A (pt) 2007-07-31
TW200540159A (en) 2005-12-16
WO2005087744A8 (en) 2006-10-26
NO20064416L (no) 2006-12-07
KR20060124783A (ko) 2006-12-05
IL177499A0 (en) 2006-12-10

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