ZA200305343B - Fumaric acid derivatives as NF-kappaB inhibitors. - Google Patents

Fumaric acid derivatives as NF-kappaB inhibitors. Download PDF

Info

Publication number: ZA200305343B
Authority: ZA; South Africa
Prior art keywords: fumaric acid; fumarate; use according; methyl; composition
Prior art date: 2001-01-12

Application number

ZA200305343A

Other languages

English (en)

Inventor

Rajendra Kumar Joshi

Peter Petzelbauer

Hans-Peter Strebel

Original Assignee

Fumapharm 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.)

2001-01-12

Filing date

2003-07-10

Publication date

2004-08-17

2003-07-10 Application filed by Fumapharm Ag filed Critical Fumapharm Ag

2004-08-17 Publication of ZA200305343B publication Critical patent/ZA200305343B/en

Links

150000002237 fumaric acid derivatives Chemical class 0.000 title claims description 20
230000017128 negative regulation of NF-kappaB transcription factor activity Effects 0.000 title description 4
VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 claims description 79
239000000203 mixture Substances 0.000 claims description 49
VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 claims description 47
239000001530 fumaric acid Substances 0.000 claims description 33
108010057466 NF-kappa B Proteins 0.000 claims description 30
-1 alkyl radical Chemical class 0.000 claims description 27
238000000034 method Methods 0.000 claims description 27
LDCRTTXIJACKKU-ONEGZZNKSA-N dimethyl fumarate Chemical compound COC(=O)\C=C\C(=O)OC LDCRTTXIJACKKU-ONEGZZNKSA-N 0.000 claims description 19
229960004419 dimethyl fumarate Drugs 0.000 claims description 18
210000004027 cell Anatomy 0.000 claims description 17
150000002148 esters Chemical class 0.000 claims description 17
229940050411 fumarate Drugs 0.000 claims description 14
239000008194 pharmaceutical composition Substances 0.000 claims description 14
150000003839 salts Chemical class 0.000 claims description 14
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239000002775 capsule Substances 0.000 claims description 12
201000010099 disease Diseases 0.000 claims description 11
208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 11
125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 11
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238000009505 enteric coating Methods 0.000 claims description 7
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150000003254 radicals Chemical class 0.000 claims description 7
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206010028980 Neoplasm Diseases 0.000 claims description 6
229910052784 alkaline earth metal Inorganic materials 0.000 claims description 6
231100000283 hepatitis Toxicity 0.000 claims description 6
125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
125000000217 alkyl group Chemical group 0.000 claims description 5
IEPRKVQEAMIZSS-AATRIKPKSA-N diethyl fumarate Chemical compound CCOC(=O)\C=C\C(=O)OCC IEPRKVQEAMIZSS-AATRIKPKSA-N 0.000 claims description 5
229920002554 vinyl polymer Polymers 0.000 claims description 5
XLYMOEINVGRTEX-ONEGZZNKSA-N (e)-4-ethoxy-4-oxobut-2-enoic acid Chemical compound CCOC(=O)\C=C\C(O)=O XLYMOEINVGRTEX-ONEGZZNKSA-N 0.000 claims description 4
125000004200 2-methoxyethyl group Chemical group [H]C([H])([H])OC([H])([H])C([H])([H])* 0.000 claims description 4
125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims description 4
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241000701044 Human gammaherpesvirus 4 Species 0.000 claims description 4
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WOONQYHBMBCNDD-SYWGCQIGSA-L calcium;(e)-4-ethoxy-4-oxobut-2-enoate Chemical compound [Ca+2].CCOC(=O)\C=C\C([O-])=O.CCOC(=O)\C=C\C([O-])=O WOONQYHBMBCNDD-SYWGCQIGSA-L 0.000 claims description 4
125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 4
125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 4
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125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 4
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239000003513 alkali Substances 0.000 claims description 3
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150000005840 aryl radicals Chemical class 0.000 claims description 3
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125000004122 cyclic group Chemical group 0.000 claims description 3
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LZSWAZSVVKHFFY-SFRQHTGFSA-L magnesium;(e)-4-methoxy-4-oxobut-2-enoate Chemical compound [Mg+2].COC(=O)\C=C\C([O-])=O.COC(=O)\C=C\C([O-])=O LZSWAZSVVKHFFY-SFRQHTGFSA-L 0.000 claims description 3
NKHAVTQWNUWKEO-NSCUHMNNSA-N monomethyl fumarate Chemical compound COC(=O)\C=C\C(O)=O NKHAVTQWNUWKEO-NSCUHMNNSA-N 0.000 claims description 3
229920006395 saturated elastomer Polymers 0.000 claims description 3
125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 3
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ZA200305343A 2001-01-12 2003-07-10 Fumaric acid derivatives as NF-kappaB inhibitors. ZA200305343B (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
DE10101307A DE10101307A1 (de)	2001-01-12	2001-01-12	Fumarsäurederivate als NF-kappaB-Inhibitor

Publications (1)

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ZA200305343B true ZA200305343B (en)	2004-08-17

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ID=7670424

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Application Number	Title	Priority Date	Filing Date
ZA200305343A ZA200305343B (en)	2001-01-12	2003-07-10	Fumaric acid derivatives as NF-kappaB inhibitors.

Country Status (22)

Country	Link
US (2)	US20040054001A1 (fr)
EP (1)	EP1408947A2 (fr)
JP (2)	JP2004528281A (fr)
CN (1)	CN1520291A (fr)
AU (1)	AU2002244638B2 (fr)
BG (1)	BG107829A (fr)
BR (1)	BR0206381A (fr)
CA (1)	CA2428075A1 (fr)
CZ (1)	CZ20031918A3 (fr)
DE (1)	DE10101307A1 (fr)
EE (1)	EE200300281A (fr)
HU (1)	HUP0302650A3 (fr)
IL (1)	IL156849A0 (fr)
MX (1)	MXPA03006248A (fr)
NO (1)	NO20031450L (fr)
NZ (1)	NZ525148A (fr)
PL (1)	PL363603A1 (fr)
RU (1)	RU2282440C2 (fr)
SK (1)	SK8252003A3 (fr)
WO (2)	WO2002055066A1 (fr)
YU (1)	YU55903A (fr)
ZA (1)	ZA200305343B (fr)

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2001
- 2001-01-12 DE DE10101307A patent/DE10101307A1/de not_active Withdrawn
- 2001-04-19 WO PCT/EP2001/004454 patent/WO2002055066A1/fr not_active Ceased
2002
- 2002-01-08 RU RU2003124751/15A patent/RU2282440C2/ru active
- 2002-01-08 CZ CZ20031918A patent/CZ20031918A3/cs unknown
- 2002-01-08 YU YU55903A patent/YU55903A/sh unknown
- 2002-01-08 IL IL15684902A patent/IL156849A0/xx unknown
- 2002-01-08 NZ NZ525148A patent/NZ525148A/en unknown
- 2002-01-08 WO PCT/EP2002/000108 patent/WO2002055067A2/fr not_active Ceased
- 2002-01-08 CN CNA02803628XA patent/CN1520291A/zh active Pending
- 2002-01-08 US US10/250,983 patent/US20040054001A1/en not_active Abandoned
- 2002-01-08 MX MXPA03006248A patent/MXPA03006248A/es not_active Application Discontinuation
- 2002-01-08 HU HU0302650A patent/HUP0302650A3/hu unknown
- 2002-01-08 BR BR0206381-6A patent/BR0206381A/pt not_active IP Right Cessation
- 2002-01-08 PL PL02363603A patent/PL363603A1/xx not_active Application Discontinuation
- 2002-01-08 AU AU2002244638A patent/AU2002244638B2/en not_active Ceased
- 2002-01-08 JP JP2002555801A patent/JP2004528281A/ja not_active Withdrawn
- 2002-01-08 EP EP02712806A patent/EP1408947A2/fr not_active Withdrawn
- 2002-01-08 SK SK825-2003A patent/SK8252003A3/sk not_active Application Discontinuation
- 2002-01-08 EE EEP200300281A patent/EE200300281A/xx unknown
- 2002-01-08 CA CA002428075A patent/CA2428075A1/fr not_active Abandoned
2003
- 2003-03-28 NO NO20031450A patent/NO20031450L/no not_active Application Discontinuation
- 2003-05-20 BG BG107829A patent/BG107829A/bg unknown
- 2003-07-10 ZA ZA200305343A patent/ZA200305343B/en unknown
2007
- 2007-08-02 US US11/833,150 patent/US20080233185A1/en not_active Abandoned
2008
- 2008-11-13 JP JP2008290821A patent/JP2009073854A/ja not_active Withdrawn

Also Published As

Publication number	Publication date
NO20031450L (no)	2003-09-12
HUP0302650A3 (en)	2009-08-28
BR0206381A (pt)	2004-08-03
PL363603A1 (en)	2004-11-29
JP2009073854A (ja)	2009-04-09
EP1408947A2 (fr)	2004-04-21
AU2002244638B2 (en)	2005-05-05
CA2428075A1 (fr)	2002-07-18
NZ525148A (en)	2006-06-30
RU2282440C2 (ru)	2006-08-27
IL156849A0 (en)	2004-02-08
WO2002055066A1 (fr)	2002-07-18
WO2002055067A3 (fr)	2004-02-26
EE200300281A (et)	2003-10-15
NO20031450D0 (no)	2003-03-28
US20040054001A1 (en)	2004-03-18
CZ20031918A3 (en)	2004-04-14
MXPA03006248A (es)	2004-04-02
CN1520291A (zh)	2004-08-11
HUP0302650A2 (hu)	2003-11-28
JP2004528281A (ja)	2004-09-16
RU2003124751A (ru)	2005-01-10
WO2002055067A2 (fr)	2002-07-18
YU55903A (sh)	2006-08-17
SK8252003A3 (en)	2003-12-02
US20080233185A1 (en)	2008-09-25
BG107829A (bg)	2004-12-30
DE10101307A1 (de)	2002-08-01

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