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1. 发明申请

WO0027828A2 2,4-DISUBSTITUTED TRIAZINE DERIVATIVES 审中-公开
标题翻译： 2,4-取代的三氮唑衍生物
公开(公告)号：WO0027828A2
公开(公告)日：2000-05-18
申请号：PCT/EP9908688
申请日：1999-11-04
申请人： JANSSEN PHARMACEUTICA NV , CORTE BART DE , JONGE MARC RENE DE , HEERES JAN , JANSSEN PAUL ADRIAAN JAN , KAVASH ROBERT W , KOYMANS LUCIEN MARIA HENRICUS , KUKLA MICHAEL JOSEPH , LUDOVICI DONALD WILLIAM , AKEN KOEN JEANNE ALFONS VAN
发明人： DE CORTE BART , DE JONGE MARC RENE , HEERES JAN , JANSSEN PAUL ADRIAAN JAN , KAVASH ROBERT W , KOYMANS LUCIEN MARIA HENRICUS , KUKLA MICHAEL JOSEPH , LUDOVICI DONALD WILLIAM , VAN AKEN KOEN JEANNE ALFONS
IPC分类号： C07D251/46 , A61K9/14 , A61K31/53 , A61P31/18 , C07D251/16 , C07D251/18 , C07D251/48 , C07D251/00
CPC分类号： A61K9/146 , Y10S977/775 , Y10S977/915
摘要： This invention concerns the use of the compounds of formula (I), the N-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a =a -a =a - forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl or substituted C1-6alkyl; each R independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, -S(=O)pR , -NH-S(=O)pR , -C(=O)R , -NHC(=O)H, -C(=O)NHNH2, -NHC(=O)R , -C(=NH)R or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is -X-R wherein R is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is -NR -, -NH-NH-, -N=N-, -O-, -C(=O)-, -CHOH-, -S-, -S(=O)- or -S(=O)2-; aryl is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.
摘要翻译：本发明涉及式（I）化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式的用途，其中-a 1 = a 2 -a 3 = a 4 - 与所连接的乙烯基形成苯基，吡啶基，嘧啶基，哒嗪基或吡嗪基; n为0〜4; 并在可能的情况下5; R 1是氢，芳基，甲酰基，C 1-6烷基羰基，C 1-6烷基，C 1-6烷氧基羰基或取代的C 1-6烷基; 每个R 2独立地是羟基，卤素，任选取代的C 1-6烷基，C 2-6烯基或C 2-6炔基，C 3-7环烷基，C 1-6烷氧基，C 1-6烷氧基羰基，羧基，氰基，硝基，氨基，单或二（ C 1-6烷基）氨基，多卤代甲基，多卤甲氧基，多卤甲硫基，-S（= O）p R 4，-NH-S（= O）p R 4，-C（= O）R 4， = O）H，-C（= O）NHNH 2，-NHC（= O）R 4，-C（= NH）R 4或5元杂环; p为1或2; L是任选取代的C 1-10烷基，C 2-10烯基，C 2-10炔基或C 3-7环烷基; 或L是-X-R 3，其中R 3是任选取代的苯基，吡啶基，嘧啶基，吡嗪基或哒嗪基; X是-NR 1 - ， - NH-NH-，-N = N-，-O-，-C（= O） - ， - CHOH-，-S-，-S（= O） - 或 - S（= O）2 - ; 芳基是任选取代的苯基; 用于制造用于治疗患有HIV（人类免疫缺陷病毒）感染的受试者的药物。

4. 发明专利

HRP20080359B1 PIRIMIDINI KOJI INHIBIRAJU REPLIKACIJU HIV-a 未知
公开(公告)号：HRP20080359B1
公开(公告)日：2016-01-01
申请号：HRP20080359
申请日：2008-07-17
申请人： JANSSEN PHARMACEUTICA NV
发明人： DE CORTE BART , DE JONGE MARC RENE , HEERES JAN , HO CHIH YUNG , JANSSEN PAUL ADRIAAN JAN , KAVASH ROBERT W , KOYMANS LUCIEN MARIA HENRICUS , KUKLA MICHAEL JOSEPH , LUDOVICI DONALD WILLIAM , VAN AKEN KOEN JEANNE ALFONS
IPC分类号： C07D239/47 , C07D239/48 , A61K20060101 , A61K31/505 , A61K31/506 , A61K31/513 , A61K31/551 , A61K31/5513 , A61K31/675 , A61K31/715 , A61P31/18 , C07D20060101 , C07D239/42 , C07D239/46 , C07D239/50 , C07D239/80 , C07D401/12 , C07D403/12
摘要： Ovaj izum odnosi se na upotrebu spojeva formule (I),njihovih N-oksida, farmaceutski prihvatljivih adicijskih soli, kvaternih amina i njihovih stereokemijski izomernih oblika, u kojoj formuli-a=a-a=a- tvori fenil, piridinil, pirimidinil, piridazinil ili pirazinil s povezanom vinilnom skupinom;n je 0 do 4, i gdje je to moguće 5;Rje vodik, aril, formil, C-alkil karbonil, C-alkil, C-alkiloksikarbonil, supstituirani C-alkil, ili supstituirani C-alkiloksi-C-alkilkarbonil;svaki od Rneovisno predstavlja hidroksi, halogen, prema potrebi supstituirani C-alkil, C-alkenil ili C-alkinil, C-cikloalkil, C-alkiloksi, C-alkiloksi-karbonil, karboksil, cijano, nitro, amino, mono- ili di-(C-alkil)amino, polihalometil, polihalometiloksi, polihalometiltio, -S(=O)R, -NH-S(=O)R, -C(=O)R, -NHC(=O)H, -C(=O)NHNH, -NHC(=O)R, -C=NH) Rili peteročlani heterociklički prsten;p je 1 ili 2;L je prema potrebi supstituirani C-alkil, C-alkenil, C-alkinil, C-cikloalkil; iliL je -X-RgdjeRje prema potrebi supstituirani fenil, piridinil, pirimidinil, pirazinil ili piridazinil;X je -NR-, -NH-NH-, -N=N-, -O-, -C(=O)-, -CHOH-, -S-, -S(=O)- ili -S(=O)-;Q je vodik, C-alkil, halogen, polihalo-C-alkil ili prema potrebi supstituirana amino skupina;Y predstavlja hidroksi, halogen, C-cikloalkil, prema potrebi supstituirani C-alkil, C-alkenil ili C-alkinil, C-alkiloksi, C-alkiloksi-karbonil, karboksil, cijano, nitro, amino, mono- ili di (C-alkil) amino, polihalo-metil, polihalometiloksi, polihalometiltio, -S(=O)R, -NH-S(=O)R, -C(=O)R, -NHC(=O)H, -C(-O)NHNH, -NHC(=O)R, -C(=NH)Rili aril;aril je prema potrebi supstituirani fenil;Het je prema potrebi supstituirani heterociklički radikal;za proizvodnju lijeka za liječenje osoba koje pate od infekcije s HIV-om (virus humane imunodeficijencije).

5. 发明专利

CA2496127C PIPERIDINYL COMPOUNDS THAT SELECTIVELY BIND INTEGRINS 未知
公开(公告)号：CA2496127C
公开(公告)日：2012-05-29
申请号：CA2496127
申请日：2003-08-15
申请人： JANSSEN PHARMACEUTICA NV
发明人： DE CORTE BART , KINNEY WILLIAM A , MARYANOFF BRUCE E , GHOSH SHYAMALI , LIU LI
IPC分类号： C07D417/04 , A61K31/4523 , A61K31/4545 , A61K31/4725 , A61K31/506 , A61K45/00 , A61K45/06 , A61K47/48 , A61L31/00 , A61P3/14 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/06 , A61P19/02 , A61P19/04 , A61P19/08 , A61P19/10 , A61P27/02 , A61P29/00 , A61P35/00 , A61P41/00 , A61P43/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D471/04
摘要： The invention is directed to piperidinyl compounds of formula (I) and (II) that selectively bind integrin receptors and methods for treating an integrin mediated disorder, wherein W, R2, Z and q are described in the application.

6. 发明专利

ES2355139T3 COMPUESTOS DE PIPERIDINILO QUE UNEN SELECTIVAMENTE A RECEPTORES DE INTEGRINAS. 未知
公开(公告)号：ES2355139T3
公开(公告)日：2011-03-23
申请号：ES03791686
申请日：2003-08-15
申请人： JANSSEN PHARMACEUTICA NV
发明人： DE CORTE BART , KINNEY WILLIAM , MARYANOFF BRUCE , GHOSH SHYAMALI , LIU LI
IPC分类号： C07D401/12 , A61K31/4523 , A61K31/4545 , A61K31/4725 , A61K31/506 , A61K45/00 , A61K45/06 , A61K47/48 , A61L31/00 , A61P3/14 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/06 , A61P19/02 , A61P19/04 , A61P19/08 , A61P19/10 , A61P27/02 , A61P29/00 , A61P35/00 , A61P41/00 , A61P43/00 , C07D401/14 , C07D405/14 , C07D417/04 , C07D471/04
摘要： Un compuesto de Fórmula (I): **(Ver fórmula)** dondeW se selecciona del grupo que consiste en -alquil(C0-C4)(R1) y -alquil(C0-C4)-fenilo (R1,R8); R1 se selecciona del grupo que consiste en -N(R4)(R6),-dihidro-1H-pirrolo[2,3-b]piridinil(R8), -tetrahidropirimi-dinil(R8), -tetrahidro-1,8-naftiridinil(R8), -tetrahidro-1H-azepino[2,3-b]piridinil(R8) y -piridinil(Rs); R4 se selecciona del grupo que consiste en hidrógeno y -alquil(C1-C8)(R7); R6 es -dihidroimidazolil(R4), -tetrahidropiridinil(R8), es -dihidroimidazolil(R4), -tetrahidropiridinil(R8), -tetrahi-dropirimidinil(R8) o -piridinil(R8); R7 es uno o dos sustituyentes seleccionados independientemente del grupo que consiste en hidrógeno, -alcoxi(C1-C8)(R9), -NH2, -NH-alquil(C1-C8)(R9), -N(alquil(C1-C8)(R9))2, -C(=O)H, -C(=O)-alquil(C1-C8)(R9), -C(=O)-NH2, -C(=O)-NH-alquil(C1-C8)(R9), -C(=O)-N(alquil(C1-C8)(R9))2, -C(=O)-NH-aril(R10), -C(=O)-cicloalquil(R10), -C(=O)-heterociclil(R10), -C(=O)-aril(R10), -C(=O)-heteroaril(R10), -CO2H, -CO2-alquil(C1-C8)(R9), -CO2-aril(R10), -C(=NH)-NH2, -SH, -S-alquil(C1-C8)(R9), -S-alquil(C1-C8)-S-alquil(C1-C8)(R9), -S-alquil(C1-C8)-alcoxi(C1-C8)(R9), -S-alquil(C1-C8)-NH-alquil(C1-C8)(R9), -SO2-alquil(C1-C8)(R9), -SO2-NH2, -SO2-NH-alquil(C1-C8)(R9), -SO2-N(alquil(C1-C8)(R9))2, -SO2-aril(R10), ciano, (halo)1-3, hidroxi, nitro, oxo, -cicloalquil(R10), -heteroci-clil(R10), -aril(R10) y -heteroaril(R10); R8 es de uno a cuatro sustituyentes seleccionados independientemente del grupo que consiste en hidrógeno, -alquil(C1-C8)(R9), -C(=O)H, -C(=O)-alquil(C1-C8)(R9), -C(=O)-NH2, -C(=O)-NH-alquil(C1-C8)(R9), -C(=O)-N(alquil(C1-C8)(R9))2, -C(=O)-NH-aril(R10), -C(=O)-cicloalquil(R10)', -C(=O)-heterociclil(R10), -C(=O)-aril(R10), -C(=O)-heteroaril(R10), -CO2H, -CO2-alquil(C1-C8)(R9), -CO2-aril(R10), -C(=NH)-NH2, -SO2-alquil(C1-C8)(R9), -SO2-NH2, -SO2-NH-alquil(C1-C8)(R9), -SO2-N(alquil(C1-C8)(R9))2, -SO2-aril(R10), -cicloalquil(R10) y -aril(R10) cuando se ancla a un átomo de nitrógeno; y, donde R8 es de uno a cuatro sustituyentes seleccionados independientemente del grupo que consiste en hidrógeno,-alquil(C1-C8)(R9),-alcoxi(C1-C8)(R9), -O-cicloalquil(R10), -O-aril(R10), -C(=O)H, -C(=O)-alquil(C1-C8)(R9), -C(=O)-NH2, -C(=O)-NH-alquil(C1-C8)(R9), -C(=O)-N(alquil(C1-C8)(R9))2, -C(=O)-NH-aril(R10), -C(=O)-cicloalquil(R10), -C(=O)-heterociclil(R10), -C(=O)-aril(R10), -C(=O)-heteroaril(R10), -CO2H, -CO2-alquil(C1-C8)(R9), -CO2-aril(R10), -C(=NH)-NH2, -SO2-alquil(C1-C8)(R9), -SO2-NH2, -SO2-NH-alquil(C1-C8)(R9), -SO2-N(alquil(C1-C8)(R9))2, -SO2-aril(R10), -SH, -S-alquil(C1-C8)(R9), -S-alquil(C1-C8)-S-alquil(C1-C8)(R9), -S-alquil(C1-C8)-alcoxi(C1-C8)(R9),-S-alquil(C1-C8)-NH-alquil(C1-C8)(R9), -NH2, -NH-alquil(C1-C8)(R9), -N(alquil(C1-C8)(R9))2, ciano, halo, hidroxi, nitro, oxo, -cicloalquil(R10), -hetorociclil(R10), -aril(R10) y -heteroaril(R10) cuando se ancla a un átomo de carbono; R9 se selecciona del grupo que consiste en hidrógeno, -alcoxi(C1-C8); -NH2, -NH-alquilo C1-C8, -N(alquil C1-C8)2, -C(=O)H, -C(=O)-NH2, -C(=O)-NH-alquilo C1-C8, -C(=O)-N(alquil C1-C8)2, -CO2H, -CO2-alquilo C1-C8, -SO2-alquilo C1-C8, -SO2-NH2, -SO2-NH-alquilo C1-C8, -SO2-N(alquil C1-C8)2, ciano, (halo)1-3, hidroxi, nitro y oxo; R10 es de uno a cuatro sustituyentes seleccionados independientemente del grupo que consiste en hidrógeno, -alquilo C1-C8, -C(=O)H, -C(=O)-alquilo C1-C8, -C(=O)-NH2, -C(=O)-NH-alquilo C1-C8, -C(=O)-N(alquil C1-C8)2, -CO2H, -CO2-alquilo C1-C4, -SO2-alquilo C1-C8, -SO2-NH2, -SO2-NH-C1-8alquilo y -SO2-N(alquil C1-C8)2 cuando se ancla a un átomo de nitrógeno; y, donde R10 es de uno a cuatro sustituyentes seleccionados independientemente del grupo que consiste en hidrógeno, -alquilo C1-C8, -alcoxi(C1-C8), -C(=O)H, -C(=O)-alquilo C1-C8, -C(=O)-NH2, -C(=O)-NH-alquilo C1-C8, -C(=O)-N(alquil C1-C8)2, -CO2H, -CO2-alquilo C1-C4, -SO2-alquilo C1-C8, -SO2-NH2, -SO2-NH-alquilo C1-C8, -SO2-N(alquil C1-C8)2, -NH2, -NH-alquilo C1-C8, -N(alquil C1-C8)2, ciano, halo, hidroxi, nitro y oxo cuando se ancla a un átomo de carbono; R2 es hidrógeno, -tetrahidropirimidinil(R8), -1,3-benzodioxolil(R8), -dihidrobenzofuranil(R8), -tetrahidroquinolinil(R8), -fenil(R8), -naftalenil(R8), -piridinil(R8), -pirimidinil(R8) o -quinolinil(R8); q se selecciona del grupo que consiste en 0,1, 2 o 3; Z se selecciona del grupo que consiste en hidroxi, -NH2, -NH-alquilo C1-C8, -N(alquil C1-C8)2, -O-alquilo C1-C8,-O-alquil(C1-C8)-OH, -O-alquil(C1-C8)alcoxi C1-C8, -O-alquil(C1-C8)carbonilalquilo C1-C8, -O-alquil(C1-C8)-CO2H, -O-alquil(C1-C8)-C(O)O-alquilo C1-C8,-O-alquil(C1-C8)-O-C(O)alquilo C1-C8,-O-C1-8alquil-NH2,-O-alquil(C1-C8)-NH-alquilo C1-C8,-O-alquil(C1-C8)-N(alquil C1-C8)2, -O-alquil(C1-C8)amida, -O-alquil(C1-C8)-C(O)-NH-alquilo C1-C8, -O-alquil(C1-C8)-C(O)-N(alquil C1-C8)2 y -NHC(O)-alquilo C1-C8; y sus sales, mezclas racémicas y enantiómeros farmacéuticamente aceptables.

9. 发明专利

CA2351203C 2,4-DISUBSTITUTED TRIAZINE DERIVATIVES WITH ANTI HIV ACTIVITY 未知
公开(公告)号：CA2351203C
公开(公告)日：2009-03-24
申请号：CA2351203
申请日：1999-11-04
申请人： JANSSEN PHARMACEUTICA NV
发明人： KOYMANS LUCIEN MARIA HENRICUS , KUKLA MICHAEL JOSEPH , HEERES JAN , JANSSEN PAUL ADRIAAN JAN , VAN AKEN KOEN JEANNE ALFONS , KAVASH ROBERT W , LUDOVICI DONALD WILLIAM , DE CORTE BART , DE JONGE MARC RENE
IPC分类号： C07D251/16 , C07D251/46 , A61K9/14 , A61K31/53 , A61P31/18 , C07D251/18 , C07D251/22 , C07D251/48
摘要： This invention concerns the use of the compounds of formula (1), the N-oxide s, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein - a1- a2-a3-a4 forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and whe re possible 5; R1 is hydrogen, aryl, formyl, C1-6alkylcarbonyl, C1-6alkyl, C1-6alkyloxycarbonyl or substituted C1-6alkyl; each R2 independently is hydroxy, halo, optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl, C3-7cycloalkyl, C1-6alkyloxy, C1- 6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono--or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, - S(=O)p R4, -NH-S(-O)p R4, -C(-O)R4, -NHC(-O)H, -C(=O)NHNH2, -NHC(-O)R4, -C(=NH)R4 or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C1-10alkyl, C2-10alkenyl, C2-10alkynyl or C3-7cycloalkyl; or L is -X-R3 wherein R3 is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is -NR1-, -NH-NH-, -N-N-, -O-, -C(=O)-, -CHOH-, -S-, -S(-O )- or -S(=O)2-; aryl is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering fr om HIV (Human Immunodeficiency Virus) infection.

10. 发明专利

CR7692A COMPUESTOS DE PIPERIDINILO QUE SE UNEN SELECTIVAMENTE A LAS INTEGRINAS 未知
公开(公告)号：CR7692A
公开(公告)日：2009-01-14
申请号：CR7692
申请日：2005-02-15
申请人： JANSSEN PHARMACEUTICA NV
发明人： DE CORTE BART , KINNIE WILLIAM A , MARYANOFF BRUCE E , GHOSH SHYAMALI , LIU LI
IPC分类号： A61K31/4523 , A61K31/4545 , A61K31/4725 , A61K31/506 , A61K45/00 , A61K45/06 , A61K47/48 , A61L31/00 , A61P3/14 , A61P9/00 , A61P9/10 , A61P11/00 , A61P13/12 , A61P17/06 , A61P19/02 , A61P19/04 , A61P19/08 , A61P19/10 , A61P27/02 , A61P29/00 , A61P35/00 , A61P41/00 , A61P43/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D417/04 , C07D471/04
摘要： Se refiere a compuestos de formula I y II: que se unen selectivamente a los receptores de la integrina y con metodos para tratar un trastorno mediado por la integrina, en donde W1 R2, Z y q son como se describio en la solicitud.

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