ZA200203204B - Substituted indoles for modulating NFKB activity. - Google Patents
Substituted indoles for modulating NFKB activity. Download PDFInfo
- Publication number
- ZA200203204B ZA200203204B ZA200203204A ZA200203204A ZA200203204B ZA 200203204 B ZA200203204 B ZA 200203204B ZA 200203204 A ZA200203204 A ZA 200203204A ZA 200203204 A ZA200203204 A ZA 200203204A ZA 200203204 B ZA200203204 B ZA 200203204B
- Authority
- ZA
- South Africa
- Prior art keywords
- alkyl
- unsubstituted
- formula
- heteroaryl
- heterocycle
- Prior art date
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- 230000000694 effects Effects 0.000 title claims 2
- 150000002475 indoles Chemical class 0.000 title description 4
- -1 phenyiglycine Chemical compound 0.000 claims description 92
- 125000000623 heterocyclic group Chemical group 0.000 claims description 60
- 125000001072 heteroaryl group Chemical group 0.000 claims description 48
- 150000003254 radicals Chemical group 0.000 claims description 48
- 125000003118 aryl group Chemical group 0.000 claims description 45
- 229910052736 halogen Inorganic materials 0.000 claims description 35
- 150000002367 halogens Chemical class 0.000 claims description 34
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 29
- 229910052739 hydrogen Inorganic materials 0.000 claims description 28
- 239000001257 hydrogen Substances 0.000 claims description 28
- 229910052757 nitrogen Inorganic materials 0.000 claims description 28
- 229910052717 sulfur Inorganic materials 0.000 claims description 28
- 150000001875 compounds Chemical class 0.000 claims description 27
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 27
- 125000000217 alkyl group Chemical group 0.000 claims description 23
- 125000001424 substituent group Chemical group 0.000 claims description 23
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- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims description 21
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 20
- 125000004434 sulfur atom Chemical group 0.000 claims description 20
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Natural products C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 claims description 18
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 18
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims description 18
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 17
- 125000004432 carbon atom Chemical group C* 0.000 claims description 17
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 17
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 17
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 15
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims description 14
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical compound N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 claims description 14
- AWJUIBRHMBBTKR-UHFFFAOYSA-N isoquinoline Chemical compound C1=NC=CC2=CC=CC=C21 AWJUIBRHMBBTKR-UHFFFAOYSA-N 0.000 claims description 14
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 11
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- 125000004122 cyclic group Chemical group 0.000 claims description 8
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- 125000002485 formyl group Chemical group [H]C(*)=O 0.000 claims description 5
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- 238000002560 therapeutic procedure Methods 0.000 claims description 5
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- 238000011275 oncology therapy Methods 0.000 description 1
- 125000004043 oxo group Chemical group O=* 0.000 description 1
- 125000006503 p-nitrobenzyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1[N+]([O-])=O)C([H])([H])* 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
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- 108060006633 protein kinase Proteins 0.000 description 1
- 125000004307 pyrazin-2-yl group Chemical group [H]C1=C([H])N=C(*)C([H])=N1 0.000 description 1
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- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 description 1
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 description 1
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- 150000003873 salicylate salts Chemical class 0.000 description 1
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Landscapes
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
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Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
DE19951360A DE19951360A1 (de) | 1999-10-26 | 1999-10-26 | Substituierte Indole |
Publications (1)
Publication Number | Publication Date |
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ZA200203204B true ZA200203204B (en) | 2002-10-23 |
Family
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Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
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ZA200203204A ZA200203204B (en) | 1999-10-26 | 2002-04-23 | Substituted indoles for modulating NFKB activity. |
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US (3) | US20030119820A1 (ja) |
EP (1) | EP1261601B1 (ja) |
JP (1) | JP3843012B2 (ja) |
KR (1) | KR100795709B1 (ja) |
CN (1) | CN1172929C (ja) |
AT (1) | ATE437867T1 (ja) |
AU (1) | AU781553B2 (ja) |
BR (1) | BR0015026B1 (ja) |
CA (1) | CA2389165C (ja) |
CY (1) | CY1110521T1 (ja) |
CZ (1) | CZ304885B6 (ja) |
DE (2) | DE19951360A1 (ja) |
DK (1) | DK1261601T3 (ja) |
EE (1) | EE05036B1 (ja) |
ES (1) | ES2329871T3 (ja) |
HK (1) | HK1049671A1 (ja) |
HR (1) | HRP20020357B1 (ja) |
HU (1) | HU229215B1 (ja) |
IL (2) | IL149272A0 (ja) |
ME (1) | ME00434B (ja) |
MX (1) | MXPA02003998A (ja) |
NO (1) | NO323952B1 (ja) |
NZ (1) | NZ518587A (ja) |
PL (1) | PL200115B1 (ja) |
PT (1) | PT1261601E (ja) |
RS (1) | RS50424B (ja) |
RU (1) | RU2255087C2 (ja) |
SI (1) | SI1261601T1 (ja) |
SK (1) | SK287116B6 (ja) |
TR (1) | TR200201144T2 (ja) |
WO (1) | WO2001030774A1 (ja) |
ZA (1) | ZA200203204B (ja) |
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CA2699568C (en) | 1999-12-24 | 2013-03-12 | Aventis Pharma Limited | Azaindoles |
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GB0115109D0 (en) | 2001-06-21 | 2001-08-15 | Aventis Pharma Ltd | Chemical compounds |
EP2335700A1 (en) * | 2001-07-25 | 2011-06-22 | Boehringer Ingelheim (Canada) Ltd. | Hepatitis C virus polymerase inhibitors with a heterobicylic structure |
EP1417200B1 (en) * | 2001-08-13 | 2010-06-02 | E.I. Du Pont De Nemours And Company | Substituted 1h-dihydropyrazoles, their preparation and use |
WO2003039545A2 (en) * | 2001-11-07 | 2003-05-15 | Millennium Pharmaceuticals, Inc. | Carboline derivatives as inhibitors of ikb in the treatment of multiple myeloma and others cancers |
US7176314B2 (en) | 2001-12-05 | 2007-02-13 | Amgen, Inc. | Inflammation modulators |
MXPA04006614A (es) | 2002-01-07 | 2004-10-04 | Eisai Co Ltd | Deazapurinas y usos de las mismas. |
ME00355B (me) | 2002-06-06 | 2010-06-30 | Ptp Group Ltd | Kristalisan polietilen tereftalat, koji sadrži silicijum, i postupak za njegovo dobijanje |
US6974870B2 (en) | 2002-06-06 | 2005-12-13 | Boehringer Ingelheim Phamaceuticals, Inc. | Substituted 3-amino-thieno [2,3-b]pyridine-2-carboxylic acid amide compounds and processes for preparing and their uses |
DE10237723A1 (de) * | 2002-08-17 | 2004-07-08 | Aventis Pharma Deutschland Gmbh | Verwendung von IKappaB-Kinase Inhibitoren in der Schmerztherapie |
US7462638B2 (en) * | 2002-08-17 | 2008-12-09 | Sanofi-Aventis Deutschland Gmbh | Use of IκB-kinase inhibitors in pain therapy |
DE10237722A1 (de) | 2002-08-17 | 2004-08-19 | Aventis Pharma Deutschland Gmbh | Indol- oder Benzimidazolderivate zur Modulation der IKappaB-Kinase |
CA2502429A1 (en) | 2002-10-31 | 2004-05-21 | Amgen Inc. | Antiinflammation agents |
US7223785B2 (en) | 2003-01-22 | 2007-05-29 | Boehringer Ingelheim International Gmbh | Viral polymerase inhibitors |
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EP1462105A1 (en) * | 2003-03-28 | 2004-09-29 | Procorde GmbH | Activation specific inhibitors of NF-kB and method of treating inflammatory processes in cardio-vascular diseases |
MXPA05010793A (es) * | 2003-04-09 | 2005-12-05 | Millennium Pharm Inc | Beta-carbolinas utiles para tratar enfermedades inflamatorias. |
US20050004164A1 (en) * | 2003-04-30 | 2005-01-06 | Caggiano Thomas J. | 2-Cyanopropanoic acid amide and ester derivatives and methods of their use |
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US7951801B2 (en) | 2004-04-09 | 2011-05-31 | Millennium Pharmaceuticals, Inc. | Beta-carbolines useful for treating inflammatory disease |
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PE20060373A1 (es) | 2004-06-24 | 2006-04-29 | Smithkline Beecham Corp | Derivados 3-piperidinil-7-carboxamida-indazol como inhibidores de la actividad cinasa de ikk2 |
PE20060748A1 (es) | 2004-09-21 | 2006-10-01 | Smithkline Beecham Corp | Derivados de indolcarboxamida como inhibidores de quinasa ikk2 |
DE102005025225A1 (de) | 2005-06-01 | 2006-12-07 | Sanofi-Aventis Deutschland Gmbh | Verfahren zur Herstellung von 2-(2-Amino-pyrimidin-4-yl)-1H-indol-5-carbonsäure-derivaten |
US8063071B2 (en) | 2007-10-31 | 2011-11-22 | GlaxoSmithKline, LLC | Chemical compounds |
UA99699C2 (ru) | 2005-06-30 | 2012-09-25 | Смитклайн Бичам Корпорейшн | Производные индолкарбоксамида и фармацевтическая композиция, которая их содержит |
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IT1271352B (it) * | 1993-04-08 | 1997-05-27 | Boehringer Ingelheim Italia | Derivati dell'indolo utili nel trattamento dei disturbi del sistema nervoso centrale |
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BR0012450B1 (pt) * | 1999-06-23 | 2011-08-23 | benzimidazóis substituìdos. | |
DE10237722A1 (de) * | 2002-08-17 | 2004-08-19 | Aventis Pharma Deutschland Gmbh | Indol- oder Benzimidazolderivate zur Modulation der IKappaB-Kinase |
US7462638B2 (en) * | 2002-08-17 | 2008-12-09 | Sanofi-Aventis Deutschland Gmbh | Use of IκB-kinase inhibitors in pain therapy |
RU2006143758A (ru) | 2004-05-12 | 2008-06-27 | Авентис Фармасьютикалз Инк. (Us) | По существу чистая 2-{[2-(2-метиламинопиримидин-4-ил)-1н-индол-5-карбонил]-амино}-3-(фенилпиридин-2-иламино)-пропионовая кислота в качестве ингибитора 1кв киназы |
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