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1. 发明专利

JP2002308872A NEW BENZOTRIAZOLE ANTI-INFLAMMATORY COMPOUND 审中-公开
公开(公告)号：JP2002308872A
公开(公告)日：2002-10-23
申请号：JP2002102969
申请日：2002-04-04
申请人： PFIZER PROD INC
发明人： LETAVIC MICHAEL ANTHONY , DOMBROSKI MARK ANTHONY , MCCLURE KIM FRANCIS , LAIRD ELLEN RUTH
IPC分类号： A61K31/4192 , A61K31/422 , A61K31/4439 , A61K31/497 , A61P9/02 , A61P9/10 , A61P29/00 , A61P35/00 , A61P37/02 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/04
摘要： PROBLEM TO BE SOLVED: To provide a new benzotriazole, an intermediate for producing the same, and a medicine composition containing the same. SOLUTION: A benzotriazole represented by formula (I), e.g. 6-[5-(4-fluoro-3- methylphenyl)-3H-imidazol-4-yl]-1-isopropyl-1H-benzotriazole, is provided. This compound is a strong inhibitor of MAP kinase, preferably p38 kinase, and is useful for curing inflammation, osteoarthritis, chronic rheumatism, cancer, reperfusion or ischemia in attack or heart attack, autoimmune disease, and other disorders.

2. 发明专利

JPH11199512A USE OF MMP-13 SELECTIVE INHIBITOR FOR THE TREATMENT OF ARTHROSIS DEFORMANS AND OTHER MMP-MEDIATED DISEASE 失效
公开(公告)号：JPH11199512A
公开(公告)日：1999-07-27
申请号：JP28954098
申请日：1998-10-12
申请人： PFIZER PROD INC
发明人： MCCLURE KIM FRANCIS , LOPRESTI-MORROW LORI LYNN , MITCHELL PETER GEOFFREY , REEVES LISA MARIE , REITER LAWRENCE ALAN , ROBINSON RALPH PELTON , YOCUM SUE ANN
IPC分类号： A61K45/00 , A61K31/00 , A61K31/16 , A61K31/165 , A61K31/18 , A61K31/34 , A61K31/35 , A61K31/351 , A61K31/4035 , A61K31/405 , A61K31/44 , A61K31/4406 , A61K31/445 , A61K31/66 , A61K31/662 , A61P19/00 , A61P19/02 , A61P29/00 , A61P35/00 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To obtain a medicine capable of treating or preventing arthrosis deformans and other collagenase 3-mediated diseases without giving systemic connective tissue toxicity, by including a selective inhibitor against collagenase 3 (matrix metha proteinase 13). SOLUTION: This medicine treats or prevents diseases and state which can be treated or prevented by selective inhibition against collagenase 3, and contains a collagenase 3 selective inhibitor. Preferably this inhibitor is 1- [4-(4- fluorophenoxy)benzenesulfonyl]-pyridine-3-ylmethylamino}-cyclopentanec arboxylic acid or the like. It is preferable to administer the active ingredient at a rate of 0.3-5 mg/kg.d. The active ingredient is generally contained in a preparation at 5-70 wt.%.

3. 发明专利

ES2263279T3 DERIVADOS DEL ACIDO HIDROXI-PIPECOLATO HIDROXAMICO COMO INHIBIDORES MMP. 未知
公开(公告)号：ES2263279T3
公开(公告)日：2006-12-01
申请号：ES99933076
申请日：1999-08-05
申请人： PFIZER PROD INC
发明人： MCCLURE KIM FRANCIS , NOE MARK CARL , LETAVIC MICHAEL ANTHONY , CHUPAK LOUIS STANLEY
IPC分类号： C07D211/60 , A61K20060101 , A61K31/435 , A61K31/443 , A61K31/445 , A61K31/4523 , A61K31/4525 , A61K31/454 , A61P1/02 , A61P1/04 , A61P3/10 , A61P9/08 , A61P11/00 , A61P11/06 , A61P17/00 , A61P19/02 , A61P19/10 , A61P25/00 , A61P25/28 , A61P27/02 , A61P31/04 , A61P31/18 , A61P35/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D20060101 , C07D211/00 , C07D211/66 , C07D211/96 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12
摘要： Un compuesto de **fórmula** en la que R1-R8 se seleccionan del grupo constituido por hidroxi, hidrógeno, halógeno, -CN, alquilo C1-C6, alquenilo C2-C6, (aril C6-C10)(alquenilo C2-C6), (heteroaril C6-C10)(alquenilo C2-C6), alquinilo C2-C6, (aril C6-C10)(alquinilo C2-C6), (heteroaril C2- C9)(alquinilo C2-C6), (alquil C1-C6)amino, (alquil C1- C6)tio, alcoxi C1-C6, perfluoro(alquilo C1-C6), arilo C6- C10, heteroarilo C2-C9, (aril C6-C10)amino, (aril C6- C10)tio, ariloxi C6-C10, (heteroaril C2-C9)amino, (heteroaril C2-C9)tio, heteroariloxi C2-C9, cicloalquilo C3- C6, (alquil C1-C6)hidroximetileno, piperidilo, (alquil C1- C6)piperidilo, (acil C1-C6)amino, (acil C1-C6)tio, aciloxi C1-C6, (alcoxi C1-C6)-(C=O)-, -CO2H, (alquil C1-C6)-NH- (C=O)- y [(alquil C1-C6)2]-N-(C=O)-; En el que dicho grupo alquilo C1-C6 está opcionalmente sustituido con uno o dos grupos seleccionados independien temente de (alquil C1-C6)tio, alcoxi C1-C6, trifluorometilo, -CN, halógeno, (arilo C6-C10), heteroarilo C2-C9,(aril C6-C10)amino, (aril C6-C10)tio, ariloxi C6- C10, (heteroaril C2-C9)amino, (heteroaril C2-C9)tio, heteroariloxi C2-C9, (aril C6-C10)(arilo C6-C10), cicloalquilo C3-C6, hidroxi, piperazinilo, (aril C6- C10)alcoxiC1-C6, (heteroaril C2-C9)alcoxiC1-C6, (acil C1- C6)amino, (acil C1-C6)tio, aciloxi C1-C6, (alquil C1- C6)sulfinilo, (aril C6-C10)sulfinilo, (alquil C1-C6)sulfoni lo, (aril C6-C10)sulfonilo, amino (alquil C1-C6)amino o (alquil C1-C6)2amino; o una de sus sales farmacéuticamente aceptables.

4. 发明专利

DE602004001676D1 未知
公开(公告)号：DE602004001676D1
公开(公告)日：2006-09-07
申请号：DE602004001676
申请日：2004-02-03
申请人： PFIZER PROD INC
发明人： BRAGANZA JOHN FREDERICK , LETAVIC ANTHONY , MCCLURE KIM FRANCIS
IPC分类号： C07D471/04 , A61K31/437 , A61K31/4745 , A61P29/00 , C07D221/00 , C07D249/00 , C07D471/02
摘要： The present invention relates to novel triazolo-pyridines of the formula wherein X is >CH 2 , >NH, sulfur, >S-O, >SO 2 or oxygen; wherein said >CH 2 and >NH may optionally be substituted with a suitable substituent; R 1 is selected from the group consisting of hydrogen, (C 1 -C 6 )alkyl and other suitable substituents; R 2 is selected from the group consisting of hydrogen, (C 1 -C 6 )alkyl and other suitable substituents; s is an integer from 0-4; R 3 is R 4 , R 5 -(NR 6 )-, R 5 -S-, R 5 -(S-O)-, R 5 -(SO 2 )-, R 5 -SO 2 -NR 6 -, R 5 -(NR 6 )-SO 2 -, R 5 -O-, R 5 -(C-O)-, R 5 -(NR 6 )-(C-O)-, R 5 -(C-O)-NR 6 -, R 5 -O-(C-O)-, R 5 -(C-O)-O-, R 5 -CR 7 -CR 8 - or R 5 -C≡C-; such that the molecular weight of R 3 is less than 500 AMU, preferably less than 250 AMU; R 4 , R 5 and R 6 are each selected from the group consisting of hydrogen, (C 1 -C 6 )alkyl and other suitable substituents; or a pharmaceutically acceptable salt thereof; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, reperfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

5. 发明专利

CA2379903C NOVEL BENZOTRIAZOLES ANTI-INFLAMMATORY COMPOUNDS 未知
公开(公告)号：CA2379903C
公开(公告)日：2006-08-01
申请号：CA2379903
申请日：2002-04-02
申请人： PFIZER PROD INC
发明人： LAIRD ELLEN RUTH , MCCLURE KIM FRANCIS , LETAVIC MICHAEL ANTHONY , DOMBROSKI MARK ANTHONY
IPC分类号： C07D413/04 , A61K31/4192 , A61K31/422 , A61K31/4439 , A61K31/497 , A61P9/02 , A61P9/10 , A61P29/00 , A61P35/00 , A61P37/02 , A61P43/00 , C07D249/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D417/04
摘要： The present invention relates to novel benzotriazoles of the formula I See formula I where Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen and where at least one of the heteroatoms atoms is nitrogen; R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; R3 is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents; s is an integer from 0-5; and to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are poten t inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

6. 发明专利

DE60210755D1 未知
公开(公告)号：DE60210755D1
公开(公告)日：2006-05-24
申请号：DE60210755
申请日：2002-02-08
申请人： PFIZER PROD INC
发明人： DOMBROSKI MARK ANTHONY , DUPLANTIER ALLEN JACOB , LAIRD ELLEN RUTH , LETAVIC MICHAEL ANTHONY , MCCLURE KIM FRANCIS
IPC分类号： C07D471/04 , A61K31/435 , A61K31/4439 , A61P1/04 , A61P3/10 , A61P9/10 , A61P13/02 , A61P19/02 , A61P19/10 , A61P21/00 , A61P25/00 , A61P25/16 , A61P25/28 , A61P29/00 , A61P31/06 , A61P39/02 , A61P43/00 , C07D221/00 , C07D249/00
摘要： The present invention relates to novel triazolo-pyridines of the formula Iwherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen;R is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents;R is selected from the group consisting of hydrogen, (C1-C6)alkyl or other suitable substituents;s is an integer from 0-5;to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

7. 发明专利

ES2251582T3 COMPUESTOS ANTIINFLAMATORIOS DE BENCIMIDAZOL. 未知
公开(公告)号：ES2251582T3
公开(公告)日：2006-05-01
申请号：ES02716257
申请日：2002-01-30
申请人： PFIZER PROD INC
发明人： DOMBROSKI MARK ANTHONY , LETAVIC , MCCLURE KIM FRANCIS
IPC分类号： A61K31/4184 , A61K31/4188 , A61K31/42 , A61K31/422 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D487/04
摘要： Un compuesto de **fórmula** en la que Het es un heteroarilo de 5 miembros opcionalmente sustituido que, cuando se toma conjuntamente con (R3)s- fenilo, se selecciona entre el grupo compuesto por 192 cada uno de R1 y R2 se selecciona independientemente entre el grupo compuesto por hidrógeno, alquilo (C1-C6), cicloalquilo (C3-C10), fenilo, heteroarilo (C1-C10) y heterociclilo (C1-C10); pudiendo estar cada uno de los sustituyentes alquilo (C1-C6), cicloalquilo (C3-C10), fenilo, heteroarilo (C1-C10) y heterociclilo (C1-C10) mencionados anteriormente, opcional e independientemente sustituido con uno a cuatro restos seleccionados independientemente entre el grupo compuesto por halo, alquilo (C1-C6), alquenilo (C2-C6), alquinilo (C2-C6), perhalo-alquilo (C1-C6), fenilo, cicloalquilo (C3-C10), heteroarilo (C1-C10), heterociclilo (C1-C10), formilo, -CN, alquil (C1-C6)-(C=O), fenil-(C=O)-, HO-(C=O)-, alquil (C1-C6)-O-(C=O)-, alquil (C1-C6)-NH-(C=O)-, [alquil (C1-C6)]2-N-(C=O)-, fenil-NH-(C=O)-, fenil-[(alquil (C1-C6))-N]-(C=O)-, -NO2, amino, alquil (C1-C6)-amino, [alquil (C1-C6)]2-amino, alquil (C1-C6)-(C=O)-NH-, alquil (C1- C6)-(C=O)-[(alquil (C1-C6))-N]-, fenil-(C=O)-NH-, fenil-(C=O)- [(alquil (C1-C6))-N]-, H2N-(C=O)-NH-, alquil (C1-C6)-HN-(C=O)- NH-, [alquil (C1-C6)]2-N-(C=O)-NH-, alquil (C1-C6)-NH-(C=O)- [(alquil (C1-C6))-N]-, [alquil (C1-C6)]2-N-(C=O)-[(alquil (C1- C6))-N]-, fenil-HN-(C=O)-NH-, (fenil)2N-(C=O)-NH-, fenil-HN- (C=O)-[(alquil (C1-C6))-N]-, (fenil-)2N-(C=O)-[(alquil (C1- C6))-N]-, alquil (C1-C6)-O-(C=O)-NH-, alquil (C1-C6)-O-(C=O)- [(alquil (C1-C6))-N]-, fenil-O-(C=O)-NH-, fenil-O-(C=O)- [(alquil (C1-C6))-N]-, alquil (C1-C6)-SO2NH-, fenil-SO2NH-, alquil (C1-C6)-SO2-, fenil-SO2-, hidroxi, alcoxi (C1-C6), perhalo-alcoxi (C1-C6), fenoxi, alquil (C1-C6)-(C=O)-O-, fenil-(C=O)-O-, H2N-(C=O)-O-, alquil (C1-C6)-HN-(C=O)-O-, [alquil (C1-C6)]2N-(C=O)-O-, fenil-HN-(C=O)-O-, y (fenil-)2N- (C=O)-O-; pudiendo tomarse dos sustituyentes adyacentes sobre dichos cicloalquilo (C3-C10),fenilo, heteroarilo (C1-C10) o heterociclilo (C1-C10) de R1 o R2, conjuntamente con el carbono o heteroátomo al que están unidos para formar un anillo carbocíclico o heterocíclico de cinco a seis miembros; conteniendo cada uno de dichos restos un fenilo que, como alternativa, puede estar opcionalmente sustituido con uno o dos radicales seleccionados independientemente entre el grupo compuesto por alquilo (C1-C6), halo, alcoxi (C1-C6), perhalo- alquilo (C1-C6) y perhalo-alcoxi (C1-C6); o una sal farmacéuticamente aceptable del mismo.

8. 发明专利

DE60207390D1 未知
公开(公告)号：DE60207390D1
公开(公告)日：2005-12-22
申请号：DE60207390
申请日：2002-01-30
申请人： PFIZER PROD INC
发明人： DOMBROSKI MARK ANTHONY , LETAVIC MICHAEL ANTHONY , MCCLURE KIM FRANCIS
IPC分类号： A61K31/4184 , A61K31/4188 , A61K31/42 , A61K31/422 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61P43/00 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/04 , C07D413/14 , C07D487/04
摘要： The present invention relates to novel triazolo-pyridines of the formula I wherein Het is an optionally substituted 5-membered heterocycle containing one to two heteroatoms selected from nitrogen, sulfur and oxygen wherein at least one of said heteroatoms atoms must be nitrogen; R 2 is selected from the group consisting of hydrogen, (C 1 -C 6 )alkyl or other suitable substituents; R 3 is selected from the group consisting of hydrogen, (C 1 -C 6 )alkyl or other suitable substituents; s is an integer from 0-5; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use. The compounds of the present invention are potent inhibitors of MAP kinases, preferably p38 kinase. They are useful in the treatment of inflammation, osteoarthritis, rheumatoid arthritis, cancer, repurfusion or ischemia in stroke or heart attack, autoimmune diseases and other disorders.

9. 发明专利

ES2202796T3 未知
公开(公告)号：ES2202796T3
公开(公告)日：2004-04-01
申请号：ES98900021
申请日：1998-01-12
申请人： PFIZER PROD INC
发明人： ROBINSON RALPH PELTON JR , MCCLURE KIM FRANCIS
IPC分类号： A61K31/18 , A61K31/4436 , A61K45/00 , A61P1/00 , A61P17/02 , A61P19/00 , A61P19/02 , A61P29/00 , A61P31/18 , A61P35/00 , A61P43/00 , C07C311/20 , C07C311/29 , C07D205/04 , C07D211/66 , C07D409/04 , A61K31/44 , A61K31/445
摘要： A compound of the formulawherein R1, R2 and Q are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, tissue ulceration, macular degeneration, restenosis, periodontal disease, epidermolysis bullosa, scleritis, and other diseases characterized by matrix metalloproteinase activity, AIDS, sepsis, septic shock and other diseases involving the production of TNF. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S) and analgesics, and in combination with cytotoxic drugs such as adriamycin, daunomycin, cis-platinum, etoposide, taxol, taxotere and other alkaloids, such as vincristine, in the treatment of cancer,

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