HUP0302173A2 - Protein kináz inhibitorokként alkalmazható pirazolvegyületek - Google Patents
Protein kináz inhibitorokként alkalmazható pirazolvegyületekInfo
- Publication number
- HUP0302173A2 HUP0302173A2 HU0302173A HUP0302173A HUP0302173A2 HU P0302173 A2 HUP0302173 A2 HU P0302173A2 HU 0302173 A HU0302173 A HU 0302173A HU P0302173 A HUP0302173 A HU P0302173A HU P0302173 A2 HUP0302173 A2 HU P0302173A2
- Authority
- HU
- Hungary
- Prior art keywords
- group
- atom
- ring
- condensed
- unsaturated
- Prior art date
Links
- 229940045988 antineoplastic drug protein kinase inhibitors Drugs 0.000 title abstract 2
- 239000003909 protein kinase inhibitor Substances 0.000 title abstract 2
- 150000003217 pyrazoles Chemical class 0.000 title 1
- -1 oxo- Chemical class 0.000 abstract 5
- 125000004429 atom Chemical group 0.000 abstract 4
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 4
- 125000001931 aliphatic group Chemical group 0.000 abstract 3
- 229910052799 carbon Inorganic materials 0.000 abstract 3
- 150000001875 compounds Chemical class 0.000 abstract 3
- 125000005842 heteroatom Chemical group 0.000 abstract 3
- 229910052757 nitrogen Inorganic materials 0.000 abstract 3
- 150000001721 carbon Chemical group 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 2
- 125000004530 1,2,4-triazinyl group Chemical group N1=NC(=NC=C1)* 0.000 abstract 1
- 102000004000 Aurora Kinase A Human genes 0.000 abstract 1
- 108090000461 Aurora Kinase A Proteins 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 102000002254 Glycogen Synthase Kinase 3 Human genes 0.000 abstract 1
- 108010014905 Glycogen Synthase Kinase 3 Proteins 0.000 abstract 1
- 102000001253 Protein Kinase Human genes 0.000 abstract 1
- 125000001118 alkylidene group Chemical group 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000825 pharmaceutical preparation Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 108060006633 protein kinase Proteins 0.000 abstract 1
- 125000003373 pyrazinyl group Chemical group 0.000 abstract 1
- 125000002098 pyridazinyl group Chemical group 0.000 abstract 1
- 125000004076 pyridyl group Chemical group 0.000 abstract 1
- 125000000714 pyrimidinyl group Chemical group 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
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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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- 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
- C07D401/12—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 chain containing hetero atoms as chain links
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- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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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
- C07D231/12—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
Abstract
A találmány a proteinkináz, különösen GSK-3 és Aurora-2 proteinkinázinhibitorokként funkcionáló általános képletű vegyületekre - amelyekképletében C gyűrű fenil-, piridil-, pirimidinil-, piridazinil-,pirazinil- vagy 1,2,4-triazinilcsoport, ahol a C gyűrű egy vagy két -R1 orto-szubsztituenst hordoz, a C gyűrűn lévő bármely más szénpozíció-R5 csoporttal szubsztituált, és adott esetben a C gyűrűn lévő kétszomszédos szubsztituens a közöttük lévő atomokkal együtt egykondenzált, telítetlen vagy részlegesen telítetlen, adott esetbenlegfeljebb három heteroatomot tartalmazó, öt- vagy hattagú gyűrűtképez, amely adott esetben halogénatommal, oxo- vagy -R8 csoporttalszubsztituált; Rx és Ry -T-R3 csoport, vagy Rx és Ry a közöttük lévőatomokkal együtt egy kondenzált, telítetlen vagy részlegesentelítetlen, adott esetben legfeljebb három heteroatomot tartalmazó, 5-8 tagú gyűrűt képez, amelyben az Rx és Ry által képezett kondenzáltgyűrűben bármely szubsztituálható szénatom oxo- vagy -T-R3 csoporttalszubsztituált, és az Rx és Ry által képezett kondenzált gyűrűbenbármely szubsztituálható nitrogénatom -R4 csoporttal szubsztituált; Tvegyértékkötés vagy alkilidénlánc; R2 és R2' -R vagy -T-W-R6 csoport,vagy R2 és R2' a közöttük lévő atomokkal együtt egy kondenzált,telítetlen vagy részlegesen telítetlen, adott esetben legfeljebb háromheteroatomot tartalmazó, 5-8 tagú gyűrűt képez, amelyben az R2 és R2'által képezett kondenzált gyűrűben bármely szubsztituálható szénatomhalogénatommal, oxo-, ciano-, nitro-, -R7 vagy -V-R6 csoporttalszubsztituált, és az R2 és R2' által képezett kondenzált gyűrűbenbármely szubsztituálható nitrogénatom -R4 csoporttal szubsztituált; R3halogénatom, -R, -OR, -C(=O)R, -CO2R, -COCOR, -COCH2COR, nitro-,ciano-, -S(O)R, -S(O)2R, -N(R7)COR, -N(R7)COO (adott esetbenszubsztituált alifás), -N(R4)N(R4)2, -C=NN(R4)2, -C=N-OR, -N(R7)CON(R7)2 , -N(R7)SO2N(R7)2, -N(R4)SO2R vagy -OC(=O) N(R7)2csoport; R hidrogénatom vagy egy adott esetben szubsztituált alifás,aril-, heteroaril- vagy heterociklilcsoport; W -C(R6)2O-, -C(R6)2S-, -C(R6)2SO-, -C(R6)2SO2-, -C(R6)2SO2-N(R6)-, -C(R6)2N(R6)-, -CO-, -CO2-,-C(R6)OC(O)-, -C(R6)O-C(O)N(R6)-, -C(R6)2N(R6)CO-, -C(R6)2N(R6)C(O)O-,-C(R6)=N-N(R6)-, -C(R6)=N-O-, -C(R6)2N(R6)N(R6)-, -C(R6)2N(R6)SO2-N(R6)-, -C(R6)2N(R6)-CON(R6)- vagy -CON(R6)- csoport; R6 hidrogénatomvagy adott esetben szubsztituált alifás csoport, vagy két ugyanazon anitrogénatomon lévő R6 csoport a nitrogénatommal heterociklil- vagyheteroarilcsoportot képez a vegyületeket tartalmazógyógyszerkészítményekre, valamint a vegyületek alkalmazási eljárásairavonatkozik. Ó
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
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US23279500P | 2000-09-15 | 2000-09-15 | |
US25788700P | 2000-12-21 | 2000-12-21 | |
US28694901P | 2001-04-27 | 2001-04-27 | |
PCT/US2001/028940 WO2002022607A1 (en) | 2000-09-15 | 2001-09-14 | Pyrazole compounds useful as protein kinase inhibitors |
Publications (1)
Publication Number | Publication Date |
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HUP0302173A2 true HUP0302173A2 (hu) | 2003-09-29 |
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Family Applications (4)
Application Number | Title | Priority Date | Filing Date |
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HU0302411A HUP0302411A2 (hu) | 2000-09-15 | 2001-09-14 | Proteinkináz inhibitorként alkalmazható pirazolvegyületek és ezeket tartalmazó gyógyszerkészítmények |
HU0302173A HUP0302173A2 (hu) | 2000-09-15 | 2001-09-14 | Protein kináz inhibitorokként alkalmazható pirazolvegyületek |
HU0302172A HUP0302172A2 (hu) | 2000-09-15 | 2001-09-14 | Protein kináz inhibitorokként alkalmazható pirazolvegyületek |
HU0401819A HUP0401819A3 (en) | 2000-09-15 | 2001-09-14 | Pyrazole compounds useful as protein kinase inhibitors and pharmaceutical compositions containing them |
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KR (4) | KR20030030005A (hu) |
CN (3) | CN1473161A (hu) |
AP (1) | AP2003002762A0 (hu) |
AT (8) | ATE327991T1 (hu) |
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IL (6) | IL154784A0 (hu) |
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- 2001-09-14 AT AT01970969T patent/ATE326458T1/de not_active IP Right Cessation
- 2001-09-14 AU AU2001290914A patent/AU2001290914A1/en not_active Abandoned
- 2001-09-14 EP EP01975210A patent/EP1317450B1/en not_active Expired - Lifetime
- 2001-09-14 KR KR10-2003-7003798A patent/KR20030032035A/ko not_active Application Discontinuation
- 2001-09-14 TW TW090122889A patent/TWI303636B/zh not_active IP Right Cessation
- 2001-09-14 AT AT01971006T patent/ATE294797T1/de active
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2003
- 2003-03-04 IL IL154747A patent/IL154747A/en not_active IP Right Cessation
- 2003-03-06 IL IL154784A patent/IL154784A/en not_active IP Right Cessation
- 2003-03-14 NO NO20031188A patent/NO20031188L/no unknown
- 2003-03-14 NO NO20031189A patent/NO326850B1/no not_active IP Right Cessation
- 2003-03-14 NO NO20031190A patent/NO20031190L/no unknown
- 2003-03-14 NO NO20031191A patent/NO327708B1/no not_active IP Right Cessation
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- 2003-11-14 HK HK03108309A patent/HK1057543A1/xx not_active IP Right Cessation
- 2003-11-20 HK HK03108474A patent/HK1057747A1/xx not_active IP Right Cessation
- 2003-11-21 HK HK03108524A patent/HK1057887A1/xx not_active IP Right Cessation
- 2003-11-25 HK HK03108588A patent/HK1057748A1/xx not_active IP Right Cessation
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- 2003-11-27 HK HK03108682A patent/HK1057702A1/xx not_active IP Right Cessation
- 2003-11-28 HK HK03108726A patent/HK1057890A1/xx not_active IP Right Cessation
- 2003-12-15 HK HK03109140A patent/HK1058356A1/xx not_active IP Right Cessation
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2006
- 2006-07-25 US US11/492,450 patent/US7951820B2/en not_active Expired - Fee Related
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2008
- 2008-01-25 JP JP2008015681A patent/JP2008115195A/ja active Pending
- 2008-12-03 AU AU2008252044A patent/AU2008252044A1/en not_active Abandoned
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2011
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