HUP0401712A2 - TNF-alfa N-heterociklusos inhibitorai és ezeket tartalmazó gyógyszerkészítmények - Google Patents
TNF-alfa N-heterociklusos inhibitorai és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0401712A2 HUP0401712A2 HU0401712A HUP0401712A HUP0401712A2 HU P0401712 A2 HUP0401712 A2 HU P0401712A2 HU 0401712 A HU0401712 A HU 0401712A HU P0401712 A HUP0401712 A HU P0401712A HU P0401712 A2 HUP0401712 A2 HU P0401712A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- substituted
- alkyl
- tnf
- carbamoyl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 abstract 2
- -1 tri-substituted phenyl group Chemical group 0.000 abstract 2
- MZOFCQQQCNRIBI-VMXHOPILSA-N (3s)-4-[[(2s)-1-[[(2s)-1-[[(1s)-1-carboxy-2-hydroxyethyl]amino]-4-methyl-1-oxopentan-2-yl]amino]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-3-[[2-[[(2s)-2,6-diaminohexanoyl]amino]acetyl]amino]-4-oxobutanoic acid Chemical compound OC[C@@H](C(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCN=C(N)N)NC(=O)[C@H](CC(O)=O)NC(=O)CNC(=O)[C@@H](N)CCCCN MZOFCQQQCNRIBI-VMXHOPILSA-N 0.000 abstract 1
- 108060008682 Tumor Necrosis Factor Proteins 0.000 abstract 1
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 abstract 1
- 239000004480 active ingredient Substances 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 125000005110 aryl thio group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 125000001434 methanylylidene group Chemical group [H]C#[*] 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 230000001575 pathological effect Effects 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 239000000651 prodrug Chemical class 0.000 abstract 1
- 229940002612 prodrug Drugs 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Abstract
A találmány tárgyát a p38 kináz működésének gátlása által acitokintermelést blokkoló, ennél fogva a kóros p38 kinázaktivitássalvagy a TNF-a expressziójával összefüggésbe hozható, főleg gyulladásosbetegségek kezelésében hasznosítható általános képletű vegyületek -ahol előnyösen W, Y és X metincsoport (=CH-) vagy nitrogénatom (=N-);Z szubsztituált amino-, N-heterociklil- vagy aril-tio-csoport; Viminocsoport vagy oxigénatom; R6 adott esetben halogénatommal, alkil-,alkoxi-, karbamoil- N-szubsztituált karbamoil- vagyheterociklilcsoporttal mono-, di- vagy triszubsztituált fenilcsoport;R6 -N (R12) (Rl3) általános képletű csoport, ahol R12 és R13együttesen 5-7 atomos, további 1-3 nitrogénatomot tartalmazó, adottesetben szubsztituált heterociklust képez; vagy R12 hidrogénatom vagyalkilcsoport, és R13 alkil- vagy szubsztituált pirrolidinilcsoport -és sóik vagy prodrug-származékaik, ezeket és adott esetben további egyvagy több hatóanyagot tartalmazó gyógyszerkészítmények és alkalmazásukképezik. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US09/891,750 US6906067B2 (en) | 1999-12-28 | 2001-06-26 | N-heterocyclic inhibitors of TNF-α expression |
| PCT/US2002/020212 WO2003002542A1 (en) | 2000-12-22 | 2002-06-25 | N-heterocyclic inhibitors of tnf-alpha expression |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0401712A2 true HUP0401712A2 (hu) | 2004-12-28 |
| HUP0401712A3 HUP0401712A3 (en) | 2009-06-29 |
Family
ID=31947149
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0401712A HUP0401712A3 (en) | 2001-06-26 | 2002-06-25 | N-heterocyclic inhibitors of tnf-alpha and pharmaceutical compositions containing them |
Country Status (7)
| Country | Link |
|---|---|
| EP (1) | EP1409463B1 (hu) |
| JP (1) | JP2004535446A (hu) |
| AT (1) | ATE458724T1 (hu) |
| CA (1) | CA2451125A1 (hu) |
| DE (1) | DE60235470D1 (hu) |
| ES (1) | ES2339226T3 (hu) |
| HU (1) | HUP0401712A3 (hu) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2006278397B2 (en) * | 2005-08-04 | 2013-01-17 | Sirtris Pharmaceuticals, Inc. | Oxazolopyridine derivatives as sirtuin modulators |
| KR101422433B1 (ko) * | 2005-12-01 | 2014-07-22 | 바스프 에스이 | 불소화 ｍ-니트로벤조일 클로라이드의 제조 방법 |
| JP2009545598A (ja) * | 2006-08-01 | 2009-12-24 | プリーシス・ファーマシューティカルズ・インコーポレイテッド | Ｐ３８キナーゼ阻害剤 |
| AR068849A1 (es) | 2007-10-12 | 2009-12-09 | Basf Se | Procedimiento para la preparacion de diamidas de acido sulfonico |
| CN102203064A (zh) * | 2008-09-02 | 2011-09-28 | 贝林格尔.英格海姆国际有限公司 | 新的苯甲酰胺，其制备及其作为药物的用途 |
| CN103347866B (zh) * | 2010-11-29 | 2016-05-18 | 加林制药公司 | 作为治疗呼吸控制不适或疾病的呼吸兴奋剂的新化合物 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NO311614B1 (no) * | 1996-10-01 | 2001-12-17 | Janssen Pharmaceutica Nv | Substituerte diamino-1,3,5-triazinderivater |
| WO1999001442A1 (en) * | 1997-07-02 | 1999-01-14 | Zeneca Limited | Triazine derivatives and their use as antibacterial agents |
| WO2001047921A1 (en) * | 1999-12-28 | 2001-07-05 | Pharmacopeia, Inc. | Pyrimidine and triazine kinase inhibitors |
-
2002
- 2002-06-25 ES ES02739978T patent/ES2339226T3/es not_active Expired - Lifetime
- 2002-06-25 CA CA002451125A patent/CA2451125A1/en not_active Abandoned
- 2002-06-25 DE DE60235470T patent/DE60235470D1/de not_active Expired - Lifetime
- 2002-06-25 JP JP2003508923A patent/JP2004535446A/ja active Pending
- 2002-06-25 AT AT02739978T patent/ATE458724T1/de not_active IP Right Cessation
- 2002-06-25 HU HU0401712A patent/HUP0401712A3/hu unknown
- 2002-06-25 EP EP02739978A patent/EP1409463B1/en not_active Expired - Lifetime
Also Published As
| Publication number | Publication date |
|---|---|
| ES2339226T3 (es) | 2010-05-18 |
| EP1409463A1 (en) | 2004-04-21 |
| ATE458724T1 (de) | 2010-03-15 |
| CA2451125A1 (en) | 2003-01-09 |
| EP1409463A4 (en) | 2004-11-17 |
| DE60235470D1 (de) | 2010-04-08 |
| JP2004535446A (ja) | 2004-11-25 |
| EP1409463B1 (en) | 2010-02-24 |
| HUP0401712A3 (en) | 2009-06-29 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA9A | Lapse of provisional patent protection due to relinquishment or protection considered relinquished |