HUP0400540A2 - 2-Pirazolin-5-on-származékok, alkalmazásuk és ezeket tartalmazó gyógyászati készítmények - Google Patents
2-Pirazolin-5-on-származékok, alkalmazásuk és ezeket tartalmazó gyógyászati készítményekInfo
- Publication number
- HUP0400540A2 HUP0400540A2 HU0400540A HUP0400540A HUP0400540A2 HU P0400540 A2 HUP0400540 A2 HU P0400540A2 HU 0400540 A HU0400540 A HU 0400540A HU P0400540 A HUP0400540 A HU P0400540A HU P0400540 A2 HUP0400540 A2 HU P0400540A2
- Authority
- HU
- Hungary
- Prior art keywords
- compounds
- nr4r5
- triazole
- imidazole
- pyridine
- Prior art date
Links
- ZRHUHDUEXWHZMA-UHFFFAOYSA-N 1,4-dihydropyrazol-5-one Chemical class O=C1CC=NN1 ZRHUHDUEXWHZMA-UHFFFAOYSA-N 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Chemical class C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 abstract 6
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical class C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 abstract 4
- 150000001875 compounds Chemical class 0.000 abstract 4
- UHOVQNZJYSORNB-UHFFFAOYSA-N Benzene Chemical compound C1=CC=CC=C1 UHOVQNZJYSORNB-UHFFFAOYSA-N 0.000 abstract 3
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical class C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 abstract 2
- KYQCOXFCLRTKLS-UHFFFAOYSA-N Pyrazine Chemical class C1=CN=CC=N1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 abstract 2
- KAESVJOAVNADME-UHFFFAOYSA-N Pyrrole Chemical compound C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 abstract 2
- SMWDFEZZVXVKRB-UHFFFAOYSA-N Quinoline Chemical class N1=CC=CC2=CC=CC=C21 SMWDFEZZVXVKRB-UHFFFAOYSA-N 0.000 abstract 2
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Chemical class COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 abstract 2
- QWENRTYMTSOGBR-UHFFFAOYSA-N 1H-1,2,3-Triazole Chemical class C=1C=NNN=1 QWENRTYMTSOGBR-UHFFFAOYSA-N 0.000 abstract 1
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical class C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 abstract 1
- HIYWOHBEPVGIQN-UHFFFAOYSA-N 1h-benzo[g]indole Chemical class C1=CC=CC2=C(NC=C3)C3=CC=C21 HIYWOHBEPVGIQN-UHFFFAOYSA-N 0.000 abstract 1
- KQBVVLOYXDVATK-UHFFFAOYSA-N 4,5,6,7-tetrahydro-1h-indole Chemical class C1CCCC2=C1C=CN2 KQBVVLOYXDVATK-UHFFFAOYSA-N 0.000 abstract 1
- NSPMIYGKQJPBQR-UHFFFAOYSA-N 4H-1,2,4-triazole Chemical class C=1N=CNN=1 NSPMIYGKQJPBQR-UHFFFAOYSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 150000001204 N-oxides Chemical class 0.000 abstract 1
- PCNDJXKNXGMECE-UHFFFAOYSA-N Phenazine Chemical class C1=CC=CC2=NC3=CC=CC=C3N=C21 PCNDJXKNXGMECE-UHFFFAOYSA-N 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003710 aryl alkyl group Chemical group 0.000 abstract 1
- SIKJAQJRHWYJAI-UHFFFAOYSA-N benzopyrrole Natural products C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 abstract 1
- 125000004432 carbon atom Chemical group C* 0.000 abstract 1
- 150000001924 cycloalkanes Chemical class 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 abstract 1
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 abstract 1
- 150000002475 indoles Chemical class 0.000 abstract 1
- ZLTPDFXIESTBQG-UHFFFAOYSA-N isothiazole Chemical compound C=1C=NSC=1 ZLTPDFXIESTBQG-UHFFFAOYSA-N 0.000 abstract 1
- CTAPFRYPJLPFDF-UHFFFAOYSA-N isoxazole Chemical compound C=1C=NOC=1 CTAPFRYPJLPFDF-UHFFFAOYSA-N 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
- 125000004953 trihalomethyl group Chemical group 0.000 abstract 1
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
- C07D401/06—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 carbon chain containing only aliphatic carbon atoms
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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A61K31/4152—1,2-Diazoles having oxo groups directly attached to the heterocyclic ring, e.g. antipyrine, phenylbutazone, sulfinpyrazone
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- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D231/18—One oxygen or sulfur atom
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- C07D401/14—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 three or more hetero rings
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- C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
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- C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
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- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Endocrinology (AREA)
- Ophthalmology & Optometry (AREA)
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Abstract
A találmány tárgyát az (I) általános képletű vegyületek, valamint ezekfiziológiailag megfelelő sói, továbbá e vegyületeket tartalmazógyógyászati készítmények képezik; a találmány tárgyához tartozik afenti vegyületek alkalmazása is gyógyászati készítményekelőállítására. Az (I) általános képletben a szubsztituensek jelentéseaz alábbi: R jelentése egy gyűrűs rendszer, például adott esetbenszubsztituált indol, imidazol, 1,2,3-triazol, 1,2,4-triazol,benzimidazol, 4,5,6,7-tetrahidroindol, benzoindol, azaindol, indazol,piridin, kinolin; R1 jelentése hidrogénatom vagy -A-Z; A jelentése -(CH2)n-, -(CH2)nNH-, (CH2)nO-, -(CH2)nS-, -(CH2)nS(O)- vagy -(CH2)nS(O)2-; Z jelentése -H, rövid szénláncú alkil-, aralkil-,trihalogénmetil-, trihalogénmetil-karboil-, R3OC(O)-, -NR4R5, -C(O)NR4R5, R3CO-, R3O- vagy egy gyűrűs rendszer, például adott esetbenszubsztituált 3-6 szénatomos cikloalkán, izoxazol, izotiazol,imidazol, benzol, pirrol, indok piridin, pirazin, vagy ezen gyűrűk N-oxid-származékai. A találmány szerinti vegyületek és ezeket tartalmazógyógyászati készítmények előnyösen alkalmazhatók egy vagy több proteinkináz aktivitásának gátlására. Ó
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US14656399P | 1999-07-30 | 1999-07-30 | |
PCT/US2000/020628 WO2001009121A2 (en) | 1999-07-30 | 2000-07-28 | 2-pyrazolin-5-ones_as tyrosine kinase inhibitors |
Publications (2)
Publication Number | Publication Date |
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HUP0400540A2 true HUP0400540A2 (hu) | 2004-06-28 |
HUP0400540A3 HUP0400540A3 (en) | 2004-09-28 |
Family
ID=22517965
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
HU0400540A HUP0400540A3 (en) | 1999-07-30 | 2000-07-28 | 2-pyrazolin-5-one derivatives, their use and pharmaceutical compositions containing them |
Country Status (21)
Country | Link |
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EP (1) | EP1218373A2 (hu) |
JP (1) | JP2003506368A (hu) |
KR (1) | KR20020091829A (hu) |
CN (1) | CN1193026C (hu) |
AR (1) | AR032279A1 (hu) |
AU (1) | AU6388900A (hu) |
BG (1) | BG106392A (hu) |
BR (1) | BR0012896A (hu) |
CA (1) | CA2380644A1 (hu) |
CZ (1) | CZ2002302A3 (hu) |
HK (1) | HK1049154A1 (hu) |
HU (1) | HUP0400540A3 (hu) |
IL (1) | IL147757A0 (hu) |
MX (1) | MXPA02001088A (hu) |
NO (1) | NO20020487L (hu) |
NZ (1) | NZ516850A (hu) |
PL (1) | PL354144A1 (hu) |
SK (1) | SK1512002A3 (hu) |
TR (1) | TR200200928T2 (hu) |
WO (1) | WO2001009121A2 (hu) |
ZA (1) | ZA200200477B (hu) |
Families Citing this family (37)
Publication number | Priority date | Publication date | Assignee | Title |
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JPH078851B2 (ja) * | 1985-07-29 | 1995-02-01 | 鐘淵化学工業株式会社 | 3−フエニルチオメチルスチレン誘導体 |
JP2678822B2 (ja) * | 1990-06-04 | 1997-11-19 | 富士写真フイルム株式会社 | ハロゲン化銀写真感光材料 |
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2000
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- 2000-07-28 NZ NZ516850A patent/NZ516850A/en unknown
- 2000-07-28 IL IL14775700A patent/IL147757A0/xx unknown
- 2000-07-28 CA CA002380644A patent/CA2380644A1/en not_active Abandoned
- 2000-07-28 CZ CZ2002302A patent/CZ2002302A3/cs unknown
- 2000-07-28 SK SK151-2002A patent/SK1512002A3/sk unknown
- 2000-07-28 PL PL00354144A patent/PL354144A1/xx not_active Application Discontinuation
- 2000-07-28 MX MXPA02001088A patent/MXPA02001088A/es unknown
- 2000-07-28 JP JP2001514324A patent/JP2003506368A/ja not_active Withdrawn
- 2000-07-28 KR KR1020027001343A patent/KR20020091829A/ko not_active Application Discontinuation
- 2000-07-28 HU HU0400540A patent/HUP0400540A3/hu unknown
- 2000-07-28 AU AU63889/00A patent/AU6388900A/en not_active Abandoned
- 2000-07-28 CN CNB008136823A patent/CN1193026C/zh not_active Expired - Fee Related
- 2000-07-28 WO PCT/US2000/020628 patent/WO2001009121A2/en not_active Application Discontinuation
- 2000-07-28 TR TR2002/00928T patent/TR200200928T2/xx unknown
- 2000-07-28 EP EP00950852A patent/EP1218373A2/en not_active Withdrawn
- 2000-07-31 AR ARP000103955A patent/AR032279A1/es unknown
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2002
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- 2002-01-30 NO NO20020487A patent/NO20020487L/no not_active Application Discontinuation
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- 2002-12-23 HK HK02109301.3A patent/HK1049154A1/zh unknown
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WO2001009121A2 (en) | 2001-02-08 |
ZA200200477B (en) | 2003-06-25 |
HK1049154A1 (zh) | 2003-05-02 |
WO2001009121A3 (en) | 2002-05-02 |
NO20020487L (no) | 2002-03-12 |
TR200200928T2 (tr) | 2002-09-23 |
BR0012896A (pt) | 2002-06-18 |
CZ2002302A3 (cs) | 2002-06-12 |
NO20020487D0 (no) | 2002-01-30 |
EP1218373A2 (en) | 2002-07-03 |
AR032279A1 (es) | 2003-11-05 |
HUP0400540A3 (en) | 2004-09-28 |
JP2003506368A (ja) | 2003-02-18 |
NZ516850A (en) | 2004-09-24 |
MXPA02001088A (es) | 2003-09-22 |
CN1193026C (zh) | 2005-03-16 |
PL354144A1 (en) | 2003-12-29 |
AU6388900A (en) | 2001-02-19 |
BG106392A (bg) | 2002-12-29 |
SK1512002A3 (en) | 2002-11-06 |
CN1377346A (zh) | 2002-10-30 |
IL147757A0 (en) | 2002-08-14 |
CA2380644A1 (en) | 2001-02-08 |
KR20020091829A (ko) | 2002-12-06 |
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