HUP0203564A2 - Heteroalkil-amino-helyettesített biciklikus nitrogén-heterociklusok mint P38 protein-kináz-inhibitorok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítmények - Google Patents
Heteroalkil-amino-helyettesített biciklikus nitrogén-heterociklusok mint P38 protein-kináz-inhibitorok, eljárás az előállításukra és ezeket tartalmazó gyógyszerkészítményekInfo
- Publication number
- HUP0203564A2 HUP0203564A2 HU0203564A HUP0203564A HUP0203564A2 HU P0203564 A2 HUP0203564 A2 HU P0203564A2 HU 0203564 A HU0203564 A HU 0203564A HU P0203564 A HUP0203564 A HU P0203564A HU P0203564 A2 HUP0203564 A2 HU P0203564A2
- Authority
- HU
- Hungary
- Prior art keywords
- optionally substituted
- group
- cycloalkyl
- alkyl
- heterosubstituted
- Prior art date
Links
- 238000002360 preparation method Methods 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 229910052757 nitrogen Inorganic materials 0.000 title 1
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 title 1
- 102000002574 p38 Mitogen-Activated Protein Kinases Human genes 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 5
- 150000001875 compounds Chemical class 0.000 abstract 5
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 abstract 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 4
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 3
- 125000001188 haloalkyl group Chemical group 0.000 abstract 3
- 125000004404 heteroalkyl group Chemical group 0.000 abstract 3
- 125000004475 heteroaralkyl group Chemical group 0.000 abstract 3
- 125000001072 heteroaryl group Chemical group 0.000 abstract 3
- 125000000623 heterocyclic group Chemical group 0.000 abstract 3
- 125000003107 substituted aryl group Chemical group 0.000 abstract 3
- 125000005346 substituted cycloalkyl group Chemical group 0.000 abstract 3
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 2
- 125000005343 heterocyclic alkyl group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 abstract 1
- 208000011231 Crohn disease Diseases 0.000 abstract 1
- 208000001132 Osteoporosis Diseases 0.000 abstract 1
- 239000012826 P38 inhibitor Substances 0.000 abstract 1
- 208000004756 Respiratory Insufficiency Diseases 0.000 abstract 1
- 206010038678 Respiratory depression Diseases 0.000 abstract 1
- 125000002252 acyl group Chemical group 0.000 abstract 1
- 125000002947 alkylene group Chemical group 0.000 abstract 1
- 206010003246 arthritis Diseases 0.000 abstract 1
- 125000004966 cyanoalkyl group Chemical group 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 125000005356 cycloalkylalkenyl group Chemical group 0.000 abstract 1
- 125000005357 cycloalkylalkynyl group Chemical group 0.000 abstract 1
- 125000005843 halogen group Chemical group 0.000 abstract 1
- 125000004474 heteroalkylene group Chemical group 0.000 abstract 1
- 208000002551 irritable bowel syndrome Diseases 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- SYSQUGFVNFXIIT-UHFFFAOYSA-N n-[4-(1,3-benzoxazol-2-yl)phenyl]-4-nitrobenzenesulfonamide Chemical class C1=CC([N+](=O)[O-])=CC=C1S(=O)(=O)NC1=CC=C(C=2OC3=CC=CC=C3N=2)C=C1 SYSQUGFVNFXIIT-UHFFFAOYSA-N 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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Abstract
A találmány (I) általános képletű vegyületekre (mely képletben R1, R2,R3, R4 és n jelentése az alábbiakban megadott), egyedi izomerjeikre,az izomerek racém vagy nem racém keverékeire és e vegyületekgyógyászatilag alkalmas sóira vonatkozik, továbbá a találmány kiterjeda vegyületek előállítási eljárására és a vegyületeket tartalmazógyógyszerkészítményekre. A találmány szerinti vegyületek p38inhibitorok és arthritis, Crohn-féle betegség, ingerlésesbélszindróma, felnőtt légzési depressziós szindróma, krónikuselzáródásos tüdőbetegség, osteoporosis vagy Alzheimer-betegségkezelésére alkalmazhatók. n értéke 0-3; R1 jelentése acilcsoport,heteroalkil-csoport, adott esetben helyettesített aril-heteroalkil-,heteroalkenil-, heteroalkinil-, heteroalkil-karbonil-,heterohelyettesített cikloalkil-, heterohelyettesítettcikloalkilalkil-, heterohelyettesített cikloalkil-alkenil-,heterohelyettesített cikloalkil-alkinil-, heteroalkil-helyettesítettcikloalkil-, adott esetben helyettesített heterociklikus, adottesetben helyettesített heterociklikus alkil-, adott esetbenheterociklikus-spiro-cikloalkil-csoport, -(alkilén)-C(O)-R11 vagy -(heteroalkilén)-C(O)-R11 csoport; R11 jelentése alkil-, halogén-alkil-, amino-, egyszeresen vagy kétszeresen helyettesített amino-,adott esetben helyettesített cikloalkil-, adott esetben helyettesítettcikloalkil-alkil-, adott esetben helyettesített aril-, adott esetbenhelyettesített aralkil-, adott esetben helyettesített heteroaril-,adott esetben helyettesített heteroaralkil-, hidroxil- vagyalkoxicsoport; R2 jelentése egymástól függetlenül alkilcsoport,halogénatom, heteroalkil- vagy vinilcsoport; R3 jelentésehidrogénatom, alkil-, heteroalkil-, adott esetben helyettesítettaril-, adott esetben helyettesített aralkil-, adott esetbenhelyettesített heteroaril-, adott esetben helyettesítettheteroaralkil-, adott esetben helyettesített cikloalkil-,cikloalkenil-, adott esetben helyettesített cikloalkil-alkil-,halogén-alkil-, ciano-alkil-, heterohelyettesített cikloalkil-,heterohelyettesített cikloalkil-alkil-, heteroalkil-helyettesítettcikloalkil-, adott esetben helyettesített heterociklikus, adottesetben helyettesített heterociklikus alkil-, -(alkilén)-C(O)R31 vagy-(heteroalkilén)-C(O)R31 csoport; R31 jelentése alkil-, halogén-alkil-, hidroxil-, alkoxi-, amino-, egyszeresen vagy kétszeresenhelyettesített amino-, adott esetben helyettesített cikloalkil-, adottesetben helyettesített cikloalkil-alkil-, adott esetben helyettesítettaril-, adott esetben helyettesített aralkil-, adott esetbenhelyettesített heteroaril- vagy adott esetben helyettesítettheteroaralkil-csoport; és R4 jelentése hidrogénatom, alkilcsoport vagy-(alkilén)-COR31 csoport] Ó
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US16080399P | 1999-10-21 | 1999-10-21 | |
| US21374300P | 2000-06-22 | 2000-06-22 | |
| PCT/EP2000/010088 WO2001029042A1 (en) | 1999-10-21 | 2000-10-13 | Heteroalkylamino-substituted bicyclic nitrogen heterocycles as inhibitors of p38 protein kinase |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0203564A2 true HUP0203564A2 (hu) | 2003-02-28 |
| HUP0203564A3 HUP0203564A3 (en) | 2004-07-28 |
Family
ID=26857240
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0203564A HUP0203564A3 (en) | 1999-10-21 | 2000-10-13 | Heteroalkylamino-substituted bicyclic nitrogen heterocycles as inhibitors of p38 protein kinease, process for their preparation and pharmaceutical compositions containing them |
Country Status (27)
| Country | Link |
|---|---|
| US (1) | US6451804B1 (hu) |
| EP (1) | EP1228070B1 (hu) |
| JP (1) | JP3961830B2 (hu) |
| KR (1) | KR100523120B1 (hu) |
| CN (1) | CN1171889C (hu) |
| AR (1) | AR026084A1 (hu) |
| AT (1) | ATE353329T1 (hu) |
| AU (1) | AU776250B2 (hu) |
| BR (1) | BR0015243A (hu) |
| CA (1) | CA2388142C (hu) |
| CZ (1) | CZ20021744A3 (hu) |
| DE (1) | DE60033307T2 (hu) |
| ES (1) | ES2280247T3 (hu) |
| HK (1) | HK1051039A1 (hu) |
| HR (1) | HRP20020328A2 (hu) |
| HU (1) | HUP0203564A3 (hu) |
| IL (1) | IL149100A0 (hu) |
| MA (1) | MA26837A1 (hu) |
| MX (1) | MXPA02003950A (hu) |
| NO (1) | NO20021781L (hu) |
| NZ (1) | NZ518119A (hu) |
| PE (1) | PE20010758A1 (hu) |
| PL (1) | PL357502A1 (hu) |
| RU (1) | RU2265606C2 (hu) |
| TR (1) | TR200201057T2 (hu) |
| WO (1) | WO2001029042A1 (hu) |
| YU (1) | YU29102A (hu) |
Families Citing this family (65)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE69939168D1 (de) | 1998-05-26 | 2008-09-04 | Warner Lambert Co | Bicyclische pyrimidine und bicyclische 3,4-dihydropyrimidine als inhibitoren der zellvermehrung |
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| GB8814352D0 (en) | 1988-06-16 | 1988-07-20 | Smith Kline French Lab | Chemical compounds |
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| TR200001079T2 (tr) * | 1997-10-20 | 2000-07-21 | F.Hoffmann-La Roche Ag | Bisiklik kinaz inhibitörleri. |
| DE69939168D1 (de) * | 1998-05-26 | 2008-09-04 | Warner Lambert Co | Bicyclische pyrimidine und bicyclische 3,4-dihydropyrimidine als inhibitoren der zellvermehrung |
| TR200101102T2 (tr) | 1998-10-23 | 2002-01-21 | F.Hoffmann-La Roche Ag | Bisiklik nitrojen heterosikleler |
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