BRPI0508481A - hidróxi-6-fenilenantridinas amido-substituìdas e seu uso como inibidores de pde4 - Google Patents
hidróxi-6-fenilenantridinas amido-substituìdas e seu uso como inibidores de pde4Info
- Publication number
- BRPI0508481A BRPI0508481A BRPI0508481-4A BRPI0508481A BRPI0508481A BR PI0508481 A BRPI0508481 A BR PI0508481A BR PI0508481 A BRPI0508481 A BR PI0508481A BR PI0508481 A BRPI0508481 A BR PI0508481A
- Authority
- BR
- Brazil
- Prior art keywords
- alkyl
- alkoxy
- hydrogen
- pde4 inhibitors
- fluorine
- Prior art date
Links
Classifications
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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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
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- 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
- A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
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- 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
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P17/06—Antipsoriatics
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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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- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
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- 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
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A—HUMAN NECESSITIES
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- A—HUMAN NECESSITIES
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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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- 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]
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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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- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
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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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- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
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- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
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- A—HUMAN NECESSITIES
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- 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
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
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- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A61P9/08—Vasodilators for multiple indications
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- 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
- C07D401/12—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 chain containing hetero atoms as chain links
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
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Abstract
HIDRóXI-6-FENILENANTRIDINAS AMIDO-SUBSTITUìDAS E SEU USO COMO INIBIDORES DA PDE4. A patente de invenção refere-se a compostos de fórmula (I) na qual, R1 é hidroxila, alcóxi C1-4, cicloalcóxi C3-7, cicloalquilmetóxi C3-7, 2,2-difluoretóxi ou alcóxi C1-4 completamente ou predominantemente substituído por flúor, R2 é hidroxila, alcóxi C1-4, cicloalcóxi C3-7, cicloalquilmetóxi C3-7, 2,2-difluoretóxi ou alcóxi C1-4 completamente ou predominantemente substituído por flúor, ou na qual R1 e R2 juntos são um grupo alquilenodióxi C1-2, R3 é hidrogênio ou alquila C1-4, R31 é hidrogênio ou alquila C1-4, um ou outro, em uma primeira modalidade (modalidade a) de acordo com a presente invenção, R4 é -O-R41, no qual R41 é hidrogênio, alquila C1-4, alcóxi C1-4-alquila C1-4, hidroxialquila C2-4, alquilcarbonila C1-7 ou aquila C1-4 completamente ou predominantemente substituída por flúor, e R5 é hidrogênio ou alquila C1-4 ou, em uma segunda modalidade (modalidade b) de acordo com a presente invenção, R4 é hidrogênio ou alquila C1-4, e R5 é -O- R51, no qual R51 é hidrogênio, alquila C1-4, alcóxi C1-4-alquila C1-4, hidroxialquila C2-4, alquilcarbonila C1-7 ou alquila C1-4 completamente ou predominantemente substituída por flúor, R6 é hidrogênio, halogênio, alquila C1-4 ou alcóxi C1-4, um ou outro, em um primeiro aspecto (aspecto 1) de acordo com a presente invenção, R7 é -N(R8)R9 ou, em um segundo aspecto (aspecto 2) de acordo com a presente invenção, R7 é -NH-N(R18)R19, são novos inibidores eficazes da PDE4.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP04100990 | 2004-03-10 | ||
EP04106677 | 2004-12-17 | ||
PCT/EP2005/051054 WO2005087745A1 (en) | 2004-03-10 | 2005-03-09 | Novel amido-substituted hydroxy-6-phenylphenanthridines and their use as pde4 inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
BRPI0508481A true BRPI0508481A (pt) | 2007-07-31 |
Family
ID=34965034
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
BRPI0508481-4A BRPI0508481A (pt) | 2004-03-10 | 2005-03-09 | hidróxi-6-fenilenantridinas amido-substituìdas e seu uso como inibidores de pde4 |
Country Status (15)
Country | Link |
---|---|
US (1) | US20070185149A1 (pt) |
EP (1) | EP1725534A1 (pt) |
JP (1) | JP2007527901A (pt) |
KR (1) | KR20060130697A (pt) |
CN (1) | CN1926113B (pt) |
AR (1) | AR049324A1 (pt) |
AU (1) | AU2005221832A1 (pt) |
BR (1) | BRPI0508481A (pt) |
CA (1) | CA2558391A1 (pt) |
IL (1) | IL177496A0 (pt) |
MX (1) | MXPA06009892A (pt) |
NO (1) | NO20064415L (pt) |
NZ (1) | NZ549254A (pt) |
TW (1) | TW200600499A (pt) |
WO (1) | WO2005087745A1 (pt) |
Families Citing this family (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1536798B1 (en) | 2002-08-29 | 2007-02-07 | ALTANA Pharma AG | 3-hydroxy-6-phenylphenanthridines as pde-4 inhibitors |
CA2495827C (en) | 2002-08-29 | 2012-05-08 | Altana Pharma Ag | 2-hydroxy-6-phenylphenanthridines as pde-4 inhibitors |
GB0316915D0 (en) | 2003-07-18 | 2003-08-20 | Glaxo Group Ltd | Compounds |
US7585872B2 (en) | 2004-02-18 | 2009-09-08 | Nycomed Gmbh | Guanidinyl-substituted hydroxy-6-phenylphenanthridines as effective phosphodiesterase (PDE) 4 inhibitors |
KR101152439B1 (ko) | 2004-03-03 | 2012-07-06 | 니코메드 게엠베하 | 신규 히드록시-6-헤테로아릴페난트리딘 및 pde4억제제로서의 이의 용도 |
AR049419A1 (es) * | 2004-03-03 | 2006-08-02 | Altana Pharma Ag | Hidroxi-6-fenilfenantridinas sustituidas con heterociclilo |
DE602005027866D1 (de) | 2004-09-08 | 2011-06-16 | Nycomed Gmbh | 3-oxa-10-aza-phenanthrene als pde4- oder pde3/4-inhibitoren |
CA2579000C (en) | 2004-09-08 | 2013-02-05 | Altana Pharma Ag | Novel 3-thia-10-aza-phenanthrene derivatives |
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 |
CA2667962A1 (en) | 2006-10-30 | 2008-05-08 | Novartis Ag | Heterocyclic compounds as antiinflammatory agents |
MX2010003155A (es) | 2007-10-04 | 2010-04-01 | Hoffmann La Roche | Derivados de ciclopropil aril amida y uso de los mismos. |
MX2010007604A (es) | 2008-01-11 | 2010-08-02 | Novartis Ag | Pirimidinas como inhibidores de cinasa. |
EP2406210A1 (en) * | 2009-03-09 | 2012-01-18 | Basf Se | Process for preparing substituted 2-nitrobiphenyls |
WO2012034095A1 (en) | 2010-09-09 | 2012-03-15 | Irm Llc | Compounds and compositions as trk inhibitors |
UY33597A (es) | 2010-09-09 | 2012-04-30 | Irm Llc | Compuestos y composiciones como inhibidores de la trk |
EP2678338B1 (en) | 2011-02-25 | 2015-09-09 | Novartis AG | Pyrazolo[1,5-a]pyridines as trk inhibitors |
Family Cites Families (25)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
ATE195867T1 (de) * | 1991-09-20 | 2000-09-15 | Glaxo Group Ltd | Neue medizinische indikation für tachykinin- antagonisten |
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 |
JP4223075B2 (ja) * | 1996-11-11 | 2009-02-12 | 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 | 気管支治療薬としてのベンゾナフチリジン |
DE69808099T2 (de) * | 1997-07-25 | 2003-05-15 | Altana Pharma Ag | Substituierte 6-alkylphenanthridine |
ES2189235T3 (es) * | 1997-07-25 | 2003-07-01 | Altana Pharma Ag | 6-fenilfenantridinas sustituidas. |
IL133824A (en) * | 1997-07-25 | 2005-12-18 | Altana Pharma Ag | Tetrazole derivatives and medicaments containing the same |
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 |
CA2359404A1 (en) * | 1999-01-15 | 2000-07-20 | Beate Gutterer | Phenanthridine-n-oxides with pde-iv inhibiting activity |
DE60024581T2 (de) * | 1999-01-15 | 2006-08-10 | Altana Pharma Ag | 6-phenylphenanthridine mit pde-iv hemmender wirkung |
ATE294793T1 (de) * | 1999-01-15 | 2005-05-15 | Altana Pharma Ag | Phenantrhridin-n-oxides mit pde-iv hemmender wirkung |
ES2236288T3 (es) * | 2000-07-14 | 2005-07-16 | Altana Pharma Ag | 6-heteroarilfenantridinas. |
SI1377574T1 (pt) * | 2001-02-21 | 2005-08-31 | Altana Pharma Ag | |
JP2005537312A (ja) * | 2002-08-17 | 2005-12-08 | アルタナ ファルマ アクチエンゲゼルシャフト | 新規のフェナントリジン |
CA2495827C (en) * | 2002-08-29 | 2012-05-08 | 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 |
AU2003277069A1 (en) * | 2002-09-30 | 2004-04-23 | Ciphergen Biosystems, Inc. | Apparatus and method for expression and capture of biomolecules and complexes on adsorbent surfaces |
AR049419A1 (es) * | 2004-03-03 | 2006-08-02 | Altana Pharma Ag | Hidroxi-6-fenilfenantridinas sustituidas con heterociclilo |
WO2005084104A2 (en) * | 2004-03-09 | 2005-09-15 | Altana Pharma Ag | Novel isoamido-substituted hydroxy-6-phenylphenanthridines and their use as pde4 inhibitors |
WO2005085203A1 (en) * | 2004-03-10 | 2005-09-15 | Altana Pharma Ag | Novel difluoroethoxy-substituted hydroxy-6-phenylphenanthridines and their use as pde4 inhibitors |
WO2005087744A1 (en) * | 2004-03-10 | 2005-09-22 | Altana Pharma Ag | Novel thio-containing hydroxy-6-phenylphenanthridines and their use as pde4 inhibitors |
ES2342728T3 (es) * | 2005-02-01 | 2010-07-13 | Nycomed Gmbh | Nuevas 6-piridilfenantridinas. |
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 |
WO2006092417A1 (en) * | 2005-03-02 | 2006-09-08 | Nycomed Gmbh | 6 -heteroaryl-1, 2, 3,4,4a, 1ob-hexahydro-phenanthridines as pde-4 inhibitors for the treatment of inflammatory disorders |
WO2006095009A1 (en) * | 2005-03-09 | 2006-09-14 | Nycomed Gmbh | Amido-substituted 6-phenylphenanthridines |
-
2005
- 2005-03-09 BR BRPI0508481-4A patent/BRPI0508481A/pt not_active IP Right Cessation
- 2005-03-09 CN CN2005800068554A patent/CN1926113B/zh not_active Expired - Fee Related
- 2005-03-09 KR KR1020067020318A patent/KR20060130697A/ko not_active Application Discontinuation
- 2005-03-09 AU AU2005221832A patent/AU2005221832A1/en not_active Abandoned
- 2005-03-09 JP JP2007502343A patent/JP2007527901A/ja not_active Withdrawn
- 2005-03-09 CA CA002558391A patent/CA2558391A1/en not_active Abandoned
- 2005-03-09 EP EP05740073A patent/EP1725534A1/en not_active Withdrawn
- 2005-03-09 NZ NZ549254A patent/NZ549254A/en unknown
- 2005-03-09 WO PCT/EP2005/051054 patent/WO2005087745A1/en active Application Filing
- 2005-03-09 US US10/591,480 patent/US20070185149A1/en not_active Abandoned
- 2005-03-09 MX MXPA06009892A patent/MXPA06009892A/es not_active Application Discontinuation
- 2005-03-10 TW TW094107344A patent/TW200600499A/zh unknown
- 2005-03-11 AR ARP050100931A patent/AR049324A1/es unknown
-
2006
- 2006-08-15 IL IL177496A patent/IL177496A0/en unknown
- 2006-09-29 NO NO20064415A patent/NO20064415L/no not_active Application Discontinuation
Also Published As
Publication number | Publication date |
---|---|
CA2558391A1 (en) | 2005-09-22 |
EP1725534A1 (en) | 2006-11-29 |
MXPA06009892A (es) | 2007-03-01 |
NO20064415L (no) | 2006-10-10 |
JP2007527901A (ja) | 2007-10-04 |
IL177496A0 (en) | 2006-12-10 |
NZ549254A (en) | 2010-06-25 |
KR20060130697A (ko) | 2006-12-19 |
AU2005221832A1 (en) | 2005-09-22 |
US20070185149A1 (en) | 2007-08-09 |
TW200600499A (en) | 2006-01-01 |
WO2005087745A8 (en) | 2006-10-26 |
AR049324A1 (es) | 2006-07-19 |
CN1926113A (zh) | 2007-03-07 |
CN1926113B (zh) | 2010-06-23 |
WO2005087745A1 (en) | 2005-09-22 |
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