AR042053A1 - Hidroxiindoles nuevos, su uso como inhibidores de la fosfodiestrasa - 4, y procesos para su preparacion - Google Patents
Hidroxiindoles nuevos, su uso como inhibidores de la fosfodiestrasa - 4, y procesos para su preparacionInfo
- Publication number
- AR042053A1 AR042053A1 ARP030104219A ARP030104219A AR042053A1 AR 042053 A1 AR042053 A1 AR 042053A1 AR P030104219 A ARP030104219 A AR P030104219A AR P030104219 A ARP030104219 A AR P030104219A AR 042053 A1 AR042053 A1 AR 042053A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- once
- aryl
- optionally substituted
- cooh
- Prior art date
Links
Classifications
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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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
- C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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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
-
- 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
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- 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
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
- C07D209/04—Indoles; Hydrogenated indoles
- C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
- C07D209/18—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
- C07D209/22—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals with an aralkyl radical attached to the ring nitrogen atom
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Health & Medical Sciences (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Virology (AREA)
- Rheumatology (AREA)
- Pulmonology (AREA)
- Cardiology (AREA)
- Tropical Medicine & Parasitology (AREA)
- Molecular Biology (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Pain & Pain Management (AREA)
- Heart & Thoracic Surgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Physical Education & Sports Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Indole Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Measuring Or Testing Involving Enzymes Or Micro-Organisms (AREA)
Abstract
Se refiere a 4- y/o 7-hidroxiindoles sustituidos, a los procesos para su preparación, a los procesos para su preparación, a las preparaciones farmacéuticas que comprenden estos compuestos y al uso farmacéutico de los mismos, los cuales son inhibidores de la fosfodiesterasa 4, como compuestos activos para el tratamiento de enfermedades sobre las cuales se puede influir mediante la utilización de los compuestos para la inhibición de la actividad de la fosfodiesterasa 4 en células inmunocomponentes (por ejemplo, macrófagos y linfocitos). Reivindicación 1: Hidroxiindoles de la general fórmula (1), en la cual: n puede ser = 1 ó 2, y R1 es i) es un alquilo C1-10, el cual es una cadena lineal o ramificada y está opcionalmente sustituido, una vez o más de una vez, por -OH, -SH, -NH2, -NH-alquilo C1-6, -N(alquilo C1-6)2, -NH-arilo C6-14, -N(arilo C6-14)2, -N(alquilo C1-6)(arilo C1-6), -NO2, -CN, -F, -Cl, -Br, -I, -O-alquilo C1-6, -O-arilo C6-14, -S-alquilo C1-6, -S-arilo C6-14, -SO3H, -SO2-alquilo C1-6, -SO2-arilo C6-14, -OSO2-alquilo C1-6, -OSO2-arilo C6-14, -COOH, -C(O)alquilo C1-5 o -O(CO)alquilo C1-5, por carbociclos mono, bi o tricíclicos saturados o monoinsaturados o poliinsaturados que presentan anillos de 3 a 14 miembros, o por heterociclos mono, bi o tricíclicos saturados o monoinsaturados o poliinsaturados que presentan anillos de 5 a 15 miembros y 1 a 6 heteroátomos los cuales son preferentemente N, O y S; donde los grupos arilo C6-14 y los sustituyentes carbocíclicos y heterocíclicos pueden, por su parte, estar opcionalmente sustituidos, una vez o más de una vez, por alquilo C1-6, -OH, -NH2, -NH-alquilo C1-6, -N(alquilo C1-6)2, -NO2, -CN, -F, -Cl, -Br, -I,. -O-alquilo C1-6, -S-alquilo C1-6, -SO3H, -SO2-alquilo C1-6, -OSO2alquilo C1-6, -COOH, -(CO)alquilo C1-6 o -O(CO)alquilo C1-6, y donde los grupos alquilo de los sustituyentes carbocíclicos y heterocíclico pueden, por su parte, estar opcionalmente sustituidos, una vez o más de una vez, por -OH, -SH, -NH2, -F, -Cl, -Br, -I, -SO3H o -COOH, o ii) es un alquenilo C2-10, el cual es monoinsaturado o poliinsaturado, de cadena lineal o ramificada y está opcionalmente sustituido, una vez o más de una vez, por -OH, -SH, -NH2, -NHalquilo C1-6, -N(alquilo C1-6)2, -NH-arilo C6-14, -N(arilo C6-14)2, -N(alquilo C1-6)(arilo C6-14), -NO2, -CN, -F, -Cl, -Br, -I, -O-alquilo C1-6, -O-arilo C6-14, -S-alquilo C1-6, -S-arilo C6-14, -SO3H, -SO2alquilo C1-6, -SO2arilo C6-14, -OSO2alquilo C1-6, -OSO2arilo C6-14, -COOH, -C(O)alquilo C1-5 o -O(CO)alquilo C1-5, por carbociclos mono, bi o tricíclicos saturados o monoinsaturados o poliinsaturados que presentan anillos de 3 a 14 miembros, o por heterociclos mono, bi o tricíclicos saturados o monoinsaturados o poliinsaturados que presentan anillos de 5 a 15 miembros y 1 a 6 heteroátomos los cuales son preferentemente N, O y S, donde los grupos arilo C6-14 y los sustituyentes carbocíclicos y heterocíclicos pueden, por su parte, estar opcionalmente sustituidos, una vez o más de una vez, por alquilo C1-6, -OH, -NH2, -NH-alquilo C1-6, -N(alquilo C1-6)2, -NO2, -CN, -F, -Cl, -Br, -I,. -O-alquilo C1-6, -S-alquilo C1-6, -SO3H, -SO2-alquilo C1-6, -OSO2alquilo C1-6, -COOH, -(CO)alquilo C1-6 o -O(CO)alquilo C1-6, y donde los grupos alquilo de los sustituyentes carbocíclicos y heterocíclico pueden, por su parte, estar opcionalmente sustituidos, una vez o más de una vez, por -OH, -SH, -NH2, -F, -Cl, -Br, -I, -SO3H o -COOH; R2 y R3 es i) son, en cada caso e independientemente uno del otro, hidrógeno o -alquilo C1-5, el cual está opcionalmente sustituido, una vez o más de una vez, por -OH, -SH, -NH2, -NHalquilo C1-6, -N(alquilo C1-6)2, -NO2, -CN, -F, -Cl, -Br, -I, -O-alquilo C1-6, -S-alquilo C1-6, -fenilo o -piridilo; -fenilo , el cual está opcionalmente sustituido, una vez o más de una vez, por -alquilo C1-3, -OH, -SH, -NH2, -NHalquilo C1-3, -N(alquilo C1-3)2, -NO2, -CN, -COOH, -COOalquilo C1-3, -F, -Cl, -Br, -I, -O-alquilo C1-3, -S-alquilo C1-3 o -O(CO)-alquilo C1-3; -piridilo, el cual está opcionalmente sustituido, una vez o más de una vez, por -alquilo C1-3, -OH, -SH, NO2, -CN, -COOH, -COOalquilo C1-3, -F, -Cl, -Br, -I, -O-alquilo C1-3, -S-alquilo C1-3 o -O(CO)-alquilo C1-3, donde sólo uno entre R2 y R3 es hidrógeno y donde los grupos alquilo en los sustituyentes carbocíclicos y heterocíclicos pueden, por su parte, estar opcionalmente sustituidos, una vez o más de una vez, por -OH, -SH, -NH2, -F, -Cl, -Br, -I, -SO3H, -COOH, -(CO)-alquilo C1-5 o -O(CO)alquilo C1-5; o ii) NR2R3 juntos forman un anillo saturado o insaturado de cinco miembros o de seis miembros el cual puede contener hasta 3 heteroátomos, preferentemente N, S y O, y el cual está opcionalmente sustituido, una vez o más de una vez, por -alquilo C1-3, -OH, -SH, -NO2, -CN, -COOH, -COOalquilo C1-6, -F, -Cl, -Br, -I, -O-alquilo C1-3, -S-alquilo C1-3 o -O(CO)-alquilo C1-3, R4 y R5 son -H o -OH, donde por los menos uno de los dos debe ser -OH, o sales de los compuestos de acuerdo con la fórmula (1).
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE10253426A DE10253426B4 (de) | 2002-11-15 | 2002-11-15 | Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung |
Publications (1)
Publication Number | Publication Date |
---|---|
AR042053A1 true AR042053A1 (es) | 2005-06-08 |
Family
ID=32240098
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP030104219A AR042053A1 (es) | 2002-11-15 | 2003-11-14 | Hidroxiindoles nuevos, su uso como inhibidores de la fosfodiestrasa - 4, y procesos para su preparacion |
Country Status (19)
Country | Link |
---|---|
US (2) | US7166637B2 (es) |
EP (1) | EP1562584A1 (es) |
JP (1) | JP2006508141A (es) |
KR (1) | KR20050075014A (es) |
CN (1) | CN1711082A (es) |
AR (1) | AR042053A1 (es) |
AU (1) | AU2003283400A1 (es) |
BR (1) | BR0316234A (es) |
CA (1) | CA2505988A1 (es) |
DE (1) | DE10253426B4 (es) |
HR (1) | HRP20050542A2 (es) |
MX (1) | MXPA05005138A (es) |
NO (1) | NO20052864L (es) |
PL (1) | PL376524A1 (es) |
RU (1) | RU2005118409A (es) |
TW (1) | TW200510306A (es) |
UA (1) | UA80567C2 (es) |
WO (1) | WO2004045607A1 (es) |
ZA (2) | ZA200503399B (es) |
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CN105770357A (zh) * | 2015-10-16 | 2016-07-20 | 北京冠瑞金生物科技有限公司 | 蒜氨酸在制备抗抑郁症药物中的用途 |
WO2017123826A1 (en) | 2016-01-14 | 2017-07-20 | Beth Israel Deaconess Medical Center, Inc. | Mast-cell modulators and uses thereof |
CN113891744A (zh) | 2019-06-10 | 2022-01-04 | 诺华股份有限公司 | 用于治疗cf、copd和支气管扩张的吡啶和吡嗪衍生物 |
KR20220052934A (ko) | 2019-08-28 | 2022-04-28 | 노파르티스 아게 | 치환 1,3-페닐 헤테로아릴 유도체 및 질환 치료에서의 이의 용도 |
Family Cites Families (11)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
NZ227841A (en) * | 1988-02-12 | 1991-08-27 | Merck Sharp & Dohme | Heterocyclic compounds with at least two non-condensed five membered rings and pharmaceutical compositions |
MX9304801A (es) * | 1992-08-06 | 1997-06-28 | Warner Lambert Co | 2-toindoles (selenoidoles) disulfuros (seleniduros) relacinados, los cuales inhiben a las proteinas tirosina cinasas y los cuales tienen propiedades anti-tumorales. |
WO1994003427A1 (en) * | 1992-08-06 | 1994-02-17 | Warner-Lambert Company | 2-thioindoles (selenoindoles) and related disulfides (selenides) which inhibit protein tyrosine kinases and which have antitumor properties |
US5567711A (en) * | 1995-04-19 | 1996-10-22 | Abbott Laboratories | Indole-3-carbonyl and indole-3-sulfonyl derivatives as platelet activating factor antagonists |
DE19636150A1 (de) * | 1996-09-06 | 1998-03-12 | Asta Medica Ag | N-substituierte Indol-3-glyoxylamide mit antiasthmatischer, antiallergischer und immunsuppressiver/immunmodulierender Wirkung |
DE19818964A1 (de) * | 1998-04-28 | 1999-11-04 | Dresden Arzneimittel | Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phospodiesterase 4 und Verfahren zu deren Herstellung |
WO1999055696A1 (de) * | 1998-04-28 | 1999-11-04 | Arzneimittelwerk Dresden Gmbh | Neue hydroxyindole, deren verwendung als inhibitoren der phosphodiesterase 4 und verfahren zu deren herstellung |
DE19917504A1 (de) * | 1999-04-17 | 2000-10-19 | Dresden Arzneimittel | Verwendung von Hydroxyindolen, die Inhibitoren der Phosphodiesterase 4 sind, zur Therapie chronisch obstruktiver Lungenerkrankungen |
DE10053275A1 (de) | 2000-10-27 | 2002-05-02 | Dresden Arzneimittel | Neue 7-Azaindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung |
TW200402417A (en) | 2002-06-21 | 2004-02-16 | Akzo Nobel Nv | 1-[(Indol-3-yl)carbonyl]piperazine derivatives |
DE10253426B4 (de) * | 2002-11-15 | 2005-09-22 | Elbion Ag | Neue Hydroxyindole, deren Verwendung als Inhibitoren der Phosphodiesterase 4 und Verfahren zu deren Herstellung |
-
2002
- 2002-11-15 DE DE10253426A patent/DE10253426B4/de not_active Expired - Fee Related
-
2003
- 2003-11-13 US US10/714,568 patent/US7166637B2/en not_active Expired - Fee Related
- 2003-11-13 TW TW092131851A patent/TW200510306A/zh unknown
- 2003-11-14 UA UAA200504467A patent/UA80567C2/uk unknown
- 2003-11-14 AR ARP030104219A patent/AR042053A1/es not_active Application Discontinuation
- 2003-11-14 JP JP2004552596A patent/JP2006508141A/ja not_active Withdrawn
- 2003-11-14 KR KR1020057008684A patent/KR20050075014A/ko not_active Application Discontinuation
- 2003-11-14 CN CNA200380103190XA patent/CN1711082A/zh active Pending
- 2003-11-14 EP EP03775355A patent/EP1562584A1/de not_active Withdrawn
- 2003-11-14 WO PCT/EP2003/012742 patent/WO2004045607A1/de active Application Filing
- 2003-11-14 RU RU2005118409/04A patent/RU2005118409A/ru not_active Application Discontinuation
- 2003-11-14 MX MXPA05005138A patent/MXPA05005138A/es active IP Right Grant
- 2003-11-14 AU AU2003283400A patent/AU2003283400A1/en not_active Abandoned
- 2003-11-14 CA CA002505988A patent/CA2505988A1/en not_active Abandoned
- 2003-11-14 BR BR0316234-6A patent/BR0316234A/pt not_active IP Right Cessation
- 2003-11-14 PL PL376524A patent/PL376524A1/pl unknown
-
2005
- 2005-04-28 ZA ZA200503399A patent/ZA200503399B/en unknown
- 2005-06-13 NO NO20052864A patent/NO20052864L/no not_active Application Discontinuation
- 2005-06-14 HR HR20050542A patent/HRP20050542A2/hr not_active Application Discontinuation
- 2005-09-01 ZA ZA200507002A patent/ZA200507002B/en unknown
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Also Published As
Publication number | Publication date |
---|---|
ZA200507002B (en) | 2006-06-28 |
KR20050075014A (ko) | 2005-07-19 |
TW200510306A (en) | 2005-03-16 |
BR0316234A (pt) | 2005-10-11 |
MXPA05005138A (es) | 2005-07-22 |
DE10253426A1 (de) | 2004-06-03 |
US20070093531A1 (en) | 2007-04-26 |
RU2005118409A (ru) | 2006-01-20 |
NO20052864L (no) | 2005-06-13 |
JP2006508141A (ja) | 2006-03-09 |
US20040147759A1 (en) | 2004-07-29 |
DE10253426B4 (de) | 2005-09-22 |
HRP20050542A2 (en) | 2005-08-31 |
WO2004045607A1 (de) | 2004-06-03 |
PL376524A1 (pl) | 2006-01-09 |
CA2505988A1 (en) | 2004-06-03 |
EP1562584A1 (de) | 2005-08-17 |
US7166637B2 (en) | 2007-01-23 |
ZA200503399B (en) | 2006-06-28 |
CN1711082A (zh) | 2005-12-21 |
UA80567C2 (en) | 2007-10-10 |
AU2003283400A1 (en) | 2004-06-15 |
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