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1. 发明申请

WO2005065416A2 PROCESS FOR THE PREPARATION OF PYRIDOPYRIMIDONES 审中-公开
标题翻译：制备吡啶并嘧啶酮的方法
公开(公告)号：WO2005065416A2
公开(公告)日：2005-07-21
申请号：PCT/US2004044064
申请日：2004-12-31
申请人： SCIOS INC , CHAKRAVARTY SARVAJIT , DUGAR SUNDEEP , TESTER RICHLAND , CONTE AURELIA
发明人： CHAKRAVARTY SARVAJIT , DUGAR SUNDEEP , TESTER RICHLAND , CONTE AURELIA
IPC分类号： C07D239/90 , C07D239/91 , C07D471/04 , C07D487/02
CPC分类号： C07D239/91 , C07D471/04
摘要： The present invention is directed to a rpocess for making 2-substituted pyridopyrimidones. In particular, 2-substituted pyridopyrimidones are made through the single step reaction of suitable acid derivatives with desired derivatives of amidines.
摘要翻译：本发明涉及制备2-取代的吡啶并嘧啶酮的方法。具体地说，2-取代的吡啶并嘧啶酮是通过合适的酸衍生物与期望的脒衍生物的单步反应制备的。

2. 发明申请

WO0246158A9 PIPERIDINE/PIPERAZINE-TYPE INHIBITORS OF P38 KINASE 审中-公开
标题翻译： P38激酶的哌啶/哌嗪类抑制剂
公开(公告)号：WO0246158A9
公开(公告)日：2003-05-01
申请号：PCT/US0143824
申请日：2001-11-20
申请人： SCIOS INC
发明人： DUGAR SUNDEEP , PERUMATTAM JOHN , TESTER RICHLAND , LU QING
IPC分类号： A61K31/454 , A61K31/4545 , A61K31/496 , A61P1/04 , A61P9/08 , A61P11/06 , A61P11/16 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/04 , C07D207/40 , C07D207/416 , C07D211/18 , C07D401/06 , C07D403/06 , C07D471/04 , C07D513/04 , A61K31/445
CPC分类号： C07D207/416 , C07D211/18 , C07D401/06 , C07D471/04 , C07D513/04
摘要： The invention is directed to inhibition of p38- alpha kinase using compounds of the formula (1) and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein: Ar is an aryl group substituted with 0-5 non-interfering substituents, wherein two adjacent noninterfering substituents can form a fused aromatic or nonaromatic ring; L and L are linkers; each R is independently a noninterfering substitutent; Z is CR or N wherein R is hydrogen or a noninterfering substituent; m is 0-4; each of n and p is an integer from 0-2 wherein the some of n and p is 0-3; Ar is a substantially planar, monocyclic or polycyclic aromatic moiety having one or more optional ring heteroatoms, said moiety being optionally substituted with one or more optional ring heteroatoms, said moiety being optionally substituted with one or more non-interfering substituents, two or more of which may form a fused ring; Z is W1-COXjY wherein Y is COR or an isotere thereof; R is a noninterfering substituent, each of W and X is a spacer of 2-6 ANGSTROM , and each of i and j is independently 0 or 1; wherein the smallest number of covalent bonds is the compound separating the atom of Ar bonded to L to the atom of Ar bonded to L is at least 6, where each of said bonds has a bond length of 1.2 to 2.0 angstroms; and/or wherein the distance in space between the atom of Ar bonded to L and the atom of Ar bonded to L is 4.5-24 angstroms; with the proviso that the protion of the compound represented by Ar -Z is not formula (2) wherein formula (3) represents a singel or double bond; n is 0-3; one Z is CA or CRA and the other is CR, CR2, NR or N; A is Wi-COXjY wherein Y is COR or an isostere thereof, each of W and X is a spacer of 2-6 ANGSTROM , and each of i and j is independently 0 ot 1; Z is NR or O; and each R independently hydrogen or a mominterfering substituent.
摘要翻译：本发明涉及使用式（1）的化合物及其药学上可接受的盐或其药物组合物抑制p38-α激酶，其中：Ar 1是被0-5个非干扰素取代的芳基取代基，其中两个相邻的非干扰取代基可以形成稠合芳族或非芳族环; L 1和L 2是接头; 每个R 1独立地是非干扰取代基; Z 1是CR 2或N，其中R 2是氢或非干扰取代基; m为0-4; n和p中的每一个是0-2的整数，其中n和p中的一些是0-3; Ar 2是具有一个或多个任选的环杂原子的基本上平面的单环或多环芳族部分，所述部分任选地被一个或多个任选的环杂原子取代，所述部分任选被一个或多个非干扰取代基取代，两个以上可以形成稠环; Z为W1-COXjY，其中Y为COR 3或其等同物; R 3是不干扰取代基，W和X各自为2-6个ANGSTROM的间隔基，i和j各自独立地为0或1; 其中最小数量的共价键是将与L 2键合的Ar 1原子连接至与L 1键合的Ar 2原子的化合物为至少6，其中每个所述键具有键长1.2-2.0埃; 和/或其中键合到L 2的Ar 1原子和与L 1键合的Ar 2原子之间的空间距离为4.5-24埃; 条件是由Ar 2 -Z表示的化合物的制备不是式（2），其中式（3）表示单键或双键; n为0-3; 一个Z <2>是CA或CRA，另一个是CR，CR2，NR或N; A是Wi-COXjY，其中Y是COR或其等同基团，W和X各自是2-6个ANGSTROM的间隔基，i和j各自独立地为0或1; Z 3为NR或O; 并且每个R独立地是氢或一个干扰的取代基。

3. 发明申请

WO2004022712A3 INDOLE-TYPE DERIVATIVES AS INHIBITORS OF p38 KINASE 审中-公开
标题翻译：作为p38激酶的抑制剂的吲哚型衍生物
公开(公告)号：WO2004022712A3
公开(公告)日：2004-04-29
申请号：PCT/US0327761
申请日：2003-09-03
申请人： SCIOS INC
发明人： CHAKRAVARTY SARVAJIT , DUGAR SUNDEEP , LU QING , LUEDTKE GREGORY R , MAVUNKEL BABU J , PERUMATAM JOHN JOSEPH , TESTER RICHLAND
IPC分类号： C07D209/18 , C07D209/42 , C07D401/06 , C07D401/14 , C07D403/06 , C07D409/12 , C07D409/14 , A61K31/496 , A61K31/454 , C07D401/10 , C07D403/10
CPC分类号： C07D401/06 , C07D209/18 , C07D209/42 , C07D401/14 , C07D403/06 , C07D409/12 , C07D409/14
摘要： The invention is directed to methods to inhibit p38-alpha kinase using compounds comprising a phenyl or thienyl coupled through a piperidine or piperazine nucleus to an indole residue wherein the indole residue mandatorily has a substituent on the ring nitrogen which is an amino or substituted amino group.
摘要翻译：本发明涉及使用包含通过哌啶或哌嗪核连接的苯基或噻吩基的化合物至吲哚残基来抑制p38-α激酶的方法，其中吲哚残基在作为氨基或取代的氨基的环氮上强制取代基。

4. 发明申请

WO0246158A2 PIPERIDINE/PIPERAZINE-TYPE INHIBITORS OF P38 KINASE 审中-公开
标题翻译： P38激酶的哌啶/哌嗪类抑制剂
公开(公告)号：WO0246158A2
公开(公告)日：2002-06-13
申请号：PCT/US0143824
申请日：2001-11-20
申请人： SCIOS INC
发明人： DUGAR SUNDEEP , PERUMATTAM JOHN , TESTER RICHLAND , LU QING
IPC分类号： A61K31/454 , A61K31/4545 , A61K31/496 , A61P1/04 , A61P9/08 , A61P11/06 , A61P11/16 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/28 , A61P29/00 , A61P31/04 , C07D207/40 , C07D207/416 , C07D211/18 , C07D401/06 , C07D403/06 , C07D471/04 , C07D513/04 , A61K31/445
CPC分类号： C07D207/416 , C07D211/18 , C07D401/06 , C07D471/04 , C07D513/04
摘要： The invention is directed to inhibition of p38- alpha kinase using compounds of the formula (1) and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein: Ar is an aryl group substituted with 0-5 non-interfering substituents, wherein two adjacent noninterfering substituents can form a fused aromatic or nonaromatic ring; L and L are linkers; each R is independently a noninterfering substitutent; Z is CR or N wherein R is hydrogen or a noninterfering substituent; m is 0-4; each of n and p is an integer from 0-2 wherein the some of n and p is 0-3; Ar is a substantially planar, monocyclic or polycyclic aromatic moiety having one or more optional ring heteroatoms, said moiety being optionally substituted with one or more optional ring heteroatoms, said moiety being optionally substituted with one or more non-interfering substituents, two or more of which may form a fused ring; Z is W1-COXjY wherein Y is COR or an isotere thereof; R is a noninterfering substituent, each of W and X is a spacer of 2-6 ANGSTROM , and each of i and j is independently 0 or 1; wherein the smallest number of covalent bonds is the compound separating the atom of Ar bonded to L to the atom of Ar bonded to L is at least 6, where each of said bonds has a bond length of 1.2 to 2.0 angstroms; and/or wherein the distance in space between the atom of Ar bonded to L and the atom of Ar bonded to L is 4.5-24 angstroms; with the proviso that the protion of the compound represented by Ar -Z is not formula (2) wherein formula (3) represents a singel or double bond; n is 0-3; one Z is CA or CRA and the other is CR, CR2, NR or N; A is Wi-COXjY wherein Y is COR or an isostere thereof, each of W and X is a spacer of 2-6 ANGSTROM , and each of i and j is independently 0 ot 1; Z is NR or O; and each R independently hydrogen or a mominterfering substituent.
摘要翻译：本发明涉及使用式（1）的化合物及其药学上可接受的盐或其药物组合物抑制p38-α激酶，其中：Ar 1是被0-5个非干扰素取代的芳基取代基，其中两个相邻的非干扰取代基可以形成稠合芳族或非芳族环; L 1和L 2是连接体; 每个R 1独立地是非干扰取代基; Z 1是CR 2或N，其中R 2是氢或非干扰取代基; m为0-4; n和p中的每一个是0-2的整数，其中n和p中的一些是0-3; Ar 2是具有一个或多个任选的环杂原子的基本上平面的单环或多环芳族部分，所述部分任选地被一个或多个任选的环杂原子取代，所述部分任选被一个或多个非干扰取代基取代，两个以上可以形成稠环; Z为W1-COXjY，其中Y为COR 3或其等同物; R 3是不干扰取代基，W和X各自为2-6个ANGSTROM的间隔基，i和j各自独立地为0或1; 其中最小数量的共价键是将与L 2键合的Ar 1原子连接至与L 1键合的Ar 2原子的化合物为至少6，其中每个所述键具有键长1.2-2.0埃; 和/或其中键合到L 2的Ar 1原子和与L 1键合的Ar 2原子之间的空间距离为4.5-24埃; 条件是由Ar 2 -Z表示的化合物的制备不是式（2），其中式（3）表示单键或双键; n为0-3; 一个Z <2>是CA或CRA，另一个是CR，CR2，NR或N; A是Wi-COXjY，其中Y是COR或其等同基团，W和X各自是2-6个ANGSTROM的间隔基，i和j各自独立地为0或1; Z 3为NR或O; 并且每个R独立地是氢或一个干扰的取代基。

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