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51. 发明专利

AT334131T 未知
公开(公告)号：AT334131T
公开(公告)日：2006-08-15
申请号：AT04707599
申请日：2004-02-03
申请人： PFIZER PROD INC
发明人： BRAGANZA JOHN FREDERICK , LETAVIC MICHAEL ANTHONY , MCCLURE KIM FRANCIS
IPC分类号： A61K31/4745 , A61P29/00 , C07D471/02 , C07D471/04 , A61K31/437 , C07D249/00 , C07D221/00
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.

52. 发明专利

CA2279276C ARYLSULFONYLAMINO HYDROXAMIC ACID DERIVATIVES 未知
公开(公告)号：CA2279276C
公开(公告)日：2005-09-13
申请号：CA2279276
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 formula (I) wherein 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.

53. 发明专利

PE20040978A1 COMPUESTOS ANTIINFLAMATORIOS DE DI Y TRIFLUORO-TRIAZOLO-PIRIDINAS 未知
公开(公告)号：PE20040978A1
公开(公告)日：2004-12-28
申请号：PE2003000863
申请日：2003-08-25
申请人： PFIZER PROD INC
发明人： DOMBROSKI MARK ANTHONY , LETAVIC MICHAEL ANTHONY , MCCLURE KIM FRANCIS
IPC分类号： A61K31/435 , A61P9/10 , A61P19/00 , A61P35/00 , C07D471/04
摘要： SE REFIERE A UN COMPUESTO DE FORMULA I DONDE R1 ES F; s ES 2-3; R2 ES CICLOALQUILO C3-C6 OPCIONALMENTE SUSTITUIDO POR HALO, ALQUILO C1-C4, OH, ENTRE OTROS, CON LA CONDICION DE QUE DICHO COMPUESTO NO PUEDE SER 6-[4-(2,4-DIFLUORO-FENIL)-OXAZOL-5-IL]-3-ISOPROPIL-[1,2,4]TRIAZOLO[4,3-a]PIRIDINA O 6-[4-(3,4-DIFLUORO-FENIL)-OXAZOL-5-IL]-3-ISOPROPIL-[1,2,4]TRIAZOLO[4,3-a]PIRIDINA. SON COMPUESTOS PREFERIDOS: 3-TERC-BUTIL-6-[4-(2,4-DIFLUORO-FENIL)-OXAZOL-5-IL]-[1,2,4]TRIAZOLO[4,3-a]PIRIDINA; 3-ISOPROPIL-6-[4-(2,3,4-TRIFLUORO-FENIL)-OXAZOL-5-IL]-[1,2,4]TRIAZOLO[4,3-a]PIRIDINA Y 3-(1-METIL-CICLOPROPIL)-6-[4-(2,4,5-TRIFLUORO-FENIL)-OXAZOL-5-IL]-[1,2,4]TRIAZOLO[4,3-a]PIRIDINA; ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA QUE INVOLUCRA DICHOS COMPUESTOS QUE SON INHIBIDORES DE LA QUINASA MAP, UTILES EN EL TRATAMIENTO DE LA INFLAMACION, OSTEOARTRITIS, CANCER, ENFERMEDADES AUTOINMUNES Y OTROS TRASTORNOS

54. 发明专利

IS1950B Arýlsúlfonýlamínó hýdroxamsýruafleiður, notkun þeirra, ásamt lyfjablöndum 未知
公开(公告)号：IS1950B
公开(公告)日：2004-10-13
申请号：IS5129
申请日：1999-07-23
申请人： PFIZER PROD INC
发明人： JR RALPH PELTON ROBINSON , 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

55. 发明专利

SK283963B6 Arylsulphonylamino hydroxamic acid derivatives 未知
公开(公告)号：SK283963B6
公开(公告)日：2004-06-08
申请号：SK101299
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 formula (I) wherein 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 characterised 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.

56. 发明专利

DK0977733T3 未知
公开(公告)号：DK0977733T3
公开(公告)日：2003-11-24
申请号：DK98900021
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,

58. 发明专利

NO20033969L 未知
公开(公告)号：NO20033969L
公开(公告)日：2003-10-13
申请号：NO20033969
申请日：2003-09-08
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： 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 , C07D471/04
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.

59. 发明专利

YU5201A DERIVATI HIDROKSIPIPEKOLATHIDROKSAMSKE KISELINE KAO INHIBITORI MMP 未知
公开(公告)号：YU5201A
公开(公告)日：2003-07-07
申请号：YU5201
申请日：1999-08-03
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： Jedinjenje formule (I): gde su R1, R2, R3, R4, R5, R6, R7, R8 i Ar kao što su prethodno definisani, kao i farmaceutski preparati koji sadrže derivate jedinjenja (I) za tretiranje stanja biranih iz grupe koju čine artritis, kancer i druga oboljenja koje karakteriše aktivnost matričnih metaloproteinaza ili reprolizina sisara. Pored toga, jedinjenja ovog pronalaska se mogu koristiti u kombinovanoj terapiji sa uobičajenim nesteroidnim anti-inflamatornim lekovima (NSAID), COX-2 inhibitorima i analgeticima, i u kombinaciji sa citotoksičnim lekovima kao što su adriamicin, daunomicin, cis-platina, etopozid, taksol, taksoter i drugim alkaoidima kao što su vinkristin, u tretmanu kancera. [A compound of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and Ar are as defined above, useful in the treatment of a condition selected from the group consisting of arthritis, cancer, and other diseases characterized by matrix metalloproteinase or mammalian reprolysin activity. In addition, the compounds of the present invention may be used in combination therapy with standard non-steroidal anti-inflammatory drugs (NSAID'S), COX-2 inhibitors 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.

60. 发明专利

BR0201087A 未知
公开(公告)号：BR0201087A
公开(公告)日：2003-05-27
申请号：BR0201087
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 , C07D403/10 , A61P19/02 , C07D407/10 , C07D417/10

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