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    Compounds and methods to treat cardiac failure and other disorders
    1.
    发明授权
    Compounds and methods to treat cardiac failure and other disorders 有权
    治疗心力衰竭和其他疾病的化合物和方法

    公开(公告)号：US07189739B2

    公开(公告)日：2007-03-13

    申请号：US10076131

    申请日：2002-02-13

    申请人： Babu J. Mavunkel ,  David Y. Liu ,  George F. Schreiner ,  John A. Lewicki ,  John J. Perumattam

    发明人： Babu J. Mavunkel ,  David Y. Liu ,  George F. Schreiner ,  John A. Lewicki ,  John J. Perumattam

    IPC分类号： A61K31/445 ,  C07D401/06

    CPC分类号： C07D401/06 ,  C07D209/08 ,  C07D209/24 ,  C07D235/06 ,  C07D401/14 ,  C07D403/06 ,  C07D471/04

    摘要： The invention is directed to compounds of the formula and the pharmaceutically acceptable salts thereof wherein Ar1 is indole, benzimidazole, or benzotriazole, optionally substituted with lower alkyl (1–4C), halo, or lower alkoxy (1–4C); X1 is CO or an isostere thereof; Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl; n is 0 or 1; Z is CH or N; X2 is CH, CH2 or an isostere thereof; and Ar2 consists of one or two phenyl moieties directly coupled to X2 and optionally substituted by halo, nitro, alkyl (1–6C), CN or CF3, or by RCO, COOR, CONR2, NR2, OR or SR, wherein R is H or alkyl (1–6C) or by phenyl, itself optionally substituted by the foregoing substituents; with the proviso that if Z is N, X1 is CO, and Ar1 is indole, Ar1 must be coupled to X1 through the 2-, 5-, 6- or 7-position. These compounds are useful in the treatment of conditions associated with inflammation. In addition, the above compounds and other compounds described herein are useful in treating conditions associated with cardiac failure.

    摘要翻译： 本发明涉及下式的化合物及其药学上可接受的盐，其中Ar 1是吲哚，苯并咪唑或苯并三唑，任选被低级烷基（1-4C），卤素或低级烷氧基（ 1-4C）; X 1是CO或其等同体; Y是任选取代的烷基，任选取代的芳基或任选取代的芳基烷基; n为0或1; Z是CH或N; X 2是CH，CH 2或它们的等离子体; 和Ar 2由一个或两个直接与X 2连接的苯基部分组成，并且任选被卤素，硝基，烷基（1-6C），CN或CF 3或RCO，COOR，CONR 2，NR 2，OR或SR，其中R是H或烷基（1-6C）或苯基 本身任选被上述取代基取代; 条件是如果Z为N，则X 1为CO，Ar 1为吲哚，则Ar 1必须与X 1 通过2-，5-，6-或7-位。 这些化合物可用于治疗与炎症相关的病症。 此外，本文所述的上述化合物和其它化合物可用于治疗与心力衰竭相关的病症。

    Compounds and methods to treat cardiac failure and other disorders
    2.
    发明授权
    Compounds and methods to treat cardiac failure and other disorders 有权
    治疗心力衰竭和其他疾病的化合物和方法

    公开(公告)号：US06340685B1

    公开(公告)日：2002-01-22

    申请号：US09275176

    申请日：1999-03-24

    申请人： Babu J. Mavunkel ,  John A. Lewicki ,  David Y. Liu ,  George F. Schreiner ,  John J. Perumattam

    发明人： Babu J. Mavunkel ,  John A. Lewicki ,  David Y. Liu ,  George F. Schreiner ,  John J. Perumattam

    IPC分类号： A61K31496

    CPC分类号： C07D235/06 ,  C07D209/08 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06

    摘要： A compound of the formula: and the pharmaceutically acceptable salts thereof, wherein each of Z1 and Z2 is independently CR4 or N; where each R4 is independently H or is alkyl (1-6C) optionally including one or more heteroatoms selected from O, S and N and optionally substituted by one or more of halo, OR, SR, NR2, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl (1-6C), or by CN or ═O, or by an aliphatic or aromatic 5 or 6 membered ring optionally containing 1-2 N heteroatoms; or two R4 taken together form a bridge optionally containing a heteroatom; R1 is  wherein X1 is CO or an isostere thereof; m is 0 or 1; Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl or two 6 taken together may form an alkyene (2-3C) bridge; n is 0 or 2; Z3 is CH or N; X2 is CH, CH2 or an isostere thereof; and Ar consists of one or two phenyl moieties directly coupled to X2 optionally substituted by halo, nitro, alkyl (1-6C), alkenyl (1-6C), CN or CF3, or by RCO, COOR, CONR2, NR2, OR, SR, OOCR or NROCR wherein R is H or alkyl (1-6C) or by phenyl, itself optionally substituted by the foregoing substituents; R2 is H, or alkyl (1-6C) optionally including one heteroatom which is O, S or N, and optionally substituted by one or more of halo, OR, SR, NR2, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl (1-6C), or by CN or ═O, or by an aliphatic or aromatic 5 or 6 membered ring optionally containing 1-2 N heteroatoms; R3 is H, halo, NO2, alkyl (1-6C), alkenyl (1-6C), CN, OR, SR, NR2, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl (1-6C).

    摘要翻译： 下式化合物及其药学上可接受的盐，其中Z 1和Z 2各自独立地为CR 4或N;其中每个R 4独立地为H或烷基（1-6C），任选地包括一个或多个选自O，S 其中R是H或烷基（1-6C），或CN或= O，或被一个或多个选自下列基团取代：卤素，OR，SR，NR2，RCO，COOR，CONR2，OOCR或NROCR， 任选含有1-2个N杂原子的脂族或芳族5或6元环; R 2一起形成任选含有杂原子的桥; R 1是其中X 1是CO或其等同体; m是0或1; Y是任选取代的烷基，任选取代的芳基或任选取代的芳烷基或两个6一起形成 烷基（2-3C）桥; n为0或2; Z3为CH或N; X2为CH，CH2或其等同基团; 并且Ar由直接连接到X2上的一个或两个苯基部分，任选被卤素，硝基，烷基（1-6C），烯基（1-6C），CN或CF 3或RCO，COOR，CONR2，NR2，OR，SR ，OOCR或NROCR，其​​中R为H或烷基（1-6C）或苯基，其本身任选被前述取代基取代; R 2为H或任选包括一个为O，S或N的杂原子的烷基（1-6C） 并且任选被一个或多个卤素，OR，SR，NR 2，RCO，COOR，CONR 2，OOCR或NROCR取代，其中R是H或烷基（1-6C），或CN或= O，或被脂族或 芳香族5或6元环，任选地含有1-2个N杂原子; R3是H，卤素，NO2，烷基（1-6C），烯基（1-6C），CN，OR，SR，NR2，RCO，COOR，CONR2， OOCR或NROCR，其​​中R是H或烷基（1-6C）。

    Compounds and methods to treat cardiac failure and other disorders
    4.
    发明授权
    Compounds and methods to treat cardiac failure and other disorders 有权
    治疗心力衰竭和其他疾病的化合物和方法

    公开(公告)号：US06448257B1

    公开(公告)日：2002-09-10

    申请号：US09535316

    申请日：2000-03-24

    申请人： Babu J. Mavunkel ,  David Y. Liu ,  George F. Schreiner ,  John A. Lewicki

    发明人： Babu J. Mavunkel ,  David Y. Liu ,  George F. Schreiner ,  John A. Lewicki

    IPC分类号： A61K31437

    CPC分类号： C07D209/08 ,  C07D209/24 ,  C07D235/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D471/04

    摘要： Compounds of the formula: wherein the dotted line represents an optional bond; and the pharmaceutically acceptable salts thereof, wherein X1 is an alkyl bridge optionally containing an O, S, or N heteroatom that forms an aliphatic 5-7 membered ring and is optionally substituted by one or more of halo, OR, SR, NR2, RCO, COOR, CONR2, OOCR, or NROCR where R is H or alkyl (1-6C), or by one or more CN or═O, or by one or more aliphatic or aromatic 5- or 6-membered rings optionally containing 1-2 heteroatoms; R1 is  wherein X2 is CO or an isostere thereof; m is 0 or 1; Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl or two Y taken together may form an alkylene (2-3C) bridge; n is 0-4; Z1 is CH or N; X3 is CH or CHR where R is H or alkyl (1-6C), or an isostere thereof; and Ar, R2 and R3 are as defined in the specification. These compounds are selective inhibitors of p38&agr; kinase.

    摘要翻译： 下式的化合物：其中虚线表示任选的键;及其药学上可接受的盐，其中X 1是任选地含有O，S或N杂原子的烷基桥，其形成脂族5-7元环并任选被取代 其中R是H或烷基（1-6C），或一个或多个CN或= O，或一个或多个卤素，OR，SR，NR 2，RCO，COOR，CONR 2，OOCR或NROCR 任选含有1-2个杂原子的脂族或芳族五元或六元环; R 1是其中X 2是CO或其等价物; m是0或1; Y是任选取代的烷基，任选取代的芳基或任选取代的芳基烷基或两个Y 一起可以形成亚烷基（2-3C）桥; n为0-4; Z1为CH或N; X3为CH或CHR，其中R为H或烷基（1-6C）或其等同体; 并且Ar，R 2和R 3如本说明书中所定义。 这些化合物是p38alpha激酶的选择性抑制剂。

    Compounds and methods to treat cardiac failure and other disorders
    6.
    发明授权
    Compounds and methods to treat cardiac failure and other disorders 有权
    治疗心力衰竭和其他疾病的化合物和方法

    公开(公告)号：US06130235A

    公开(公告)日：2000-10-10

    申请号：US128137

    申请日：1998-08-03

    申请人： Babu J. Mavunkel ,  John A. Lewicki ,  David Y. Liu ,  George F. Schreiner

    发明人： Babu J. Mavunkel ,  John A. Lewicki ,  David Y. Liu ,  George F. Schreiner

    IPC分类号： C07D209/08 ,  C07D235/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  A61K31/445

    CPC分类号： C07D209/08 ,  C07D235/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06

    摘要： The invention is directed to compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof wherein Ar.sup.1 is indole, benzimidazole, or benzotriazole, optionally substituted with lower alkyl (1-4C), halo, or lower alkoxy (1-4C);X.sup.1 is CO or an isostere thereof;Y is optionally substituted alkyl, optionally substituted aryl, or optionally substituted arylalkyl;n is 0 or 1;Z is CH or N;X.sup.2 is CH, CH.sub.2 or an isostere thereof; andAr.sup.2 consists of one or two phenyl moieties directly coupled to X.sup.2 and optionally substituted by halo, nitro, alkyl (1-6C), CN or CF.sub.3, or by RCO, COOR, CONR.sub.2, NR.sub.2, OR or SR, wherein R is H or alkyl (1-6C) or by phenyl, itself optionally substituted by the foregoing substituents;with the proviso that if Z is N, X.sup.1 is CO, and Ar.sup.1 is indole, Ar.sup.1 must be coupled to X.sup.1 through the 2-, 5-, 6- or 7-position.These compounds are useful in the treatment of conditions associated with inflammation. In addition, the above compounds and other compounds described herein are useful in treating conditions associated with cardiac failure.

    摘要翻译： 本发明涉及下式的化合物及其药学上可接受的盐，其中Ar 1是任选被低级烷基（1-4C），卤素或低级烷氧基（1-4C）取代的吲哚，苯并咪唑或苯并三唑; X1是CO或其等离子体; Y是任选取代的烷基，任选取代的芳基或任选取代的芳基烷基; n为0或1; Z是CH或N; X 2是CH，CH 2或其等价物; 并且Ar 2由直接与X 2连接并任选被卤素，硝基，烷基（1-6C），CN或CF 3或RCO，COOR，CONR2，NR2，OR或SR取代的一个或两个苯基部分组成，其中R为H 或烷基（1-6C）或苯基，其本身任选被上述取代基取代; 条件是如果Z是N，则X1是CO，Ar1是吲哚，Ar1必须通过2-，5-，6-或7-位与X1连接。 这些化合物可用于治疗与炎症相关的病症。 此外，本文所述的上述化合物和其它化合物可用于治疗与心力衰竭相关的病症。

    Quinazoline derivatives as medicaments
    9.
    发明授权
    Quinazoline derivatives as medicaments 有权
    喹唑啉衍生物作为药物

    公开(公告)号：US06277989B1

    公开(公告)日：2001-08-21

    申请号：US09525034

    申请日：2000-03-14

    申请人： Sarvajit Chakravarty ,  Sundeep Dugar ,  John J. Perumattam ,  George F. Schreiner ,  David Y. Liu ,  John A. Lewicki

    发明人： Sarvajit Chakravarty ,  Sundeep Dugar ,  John J. Perumattam ,  George F. Schreiner ,  David Y. Liu ,  John A. Lewicki

    IPC分类号： C07D23942

    CPC分类号： C07D401/12 ,  A61K31/519 ,  C07D239/94 ,  C07D471/04

    摘要： The invention is directed to methods to inhibit TGF-&bgr; and/or p38-&agr; kinase using compounds of the formula or the pharmaceutically acceptable salts thereof wherein R3 is a noninterfering substituent; each Z is CR2 or N, wherein no more than two Z positions in ring A are N, and wherein two adjacent Z positions in ring A cannot be N; each R2 is independently a noninterfering substituent; L is a linker; n is 0 or 1; and Ar′ is the residue of a cyclic aliphatic, cyclic heteroaliphatic, aromatic or heteroaromatic moiety optionally substituted with 1-3 noninterfering substituents.

    摘要翻译： 本发明涉及使用下式的化合物或其药学上可接受的盐抑制TGF-β和/或p38-α激酶的方法，其中R3是不干扰取代基;每个Z是CR2或N，其中环中不超过两个Z位置 A是N，并且其中环A中的两个相邻Z位不能是N;每个R2独立地是非干扰取代基; L是连接基; n是0或1; 并且Ar'是任选被1-3个非干扰取代基取代的环状脂族，环状杂脂族，芳族或杂芳族部分的残基。

    Quinazoline derivatives as inhibitors of P-38 &agr;
    10.
    发明授权
    Quinazoline derivatives as inhibitors of P-38 &agr; 有权
    喹唑啉衍生物作为P-38α的抑制剂

    公开(公告)号：US06184226B2

    公开(公告)日：2001-02-06

    申请号：US09141916

    申请日：1998-08-28

    申请人： Sarvajit Chakravarty ,  John J. Perumattam ,  George F. Schreiner ,  David Y. Liu ,  John A. Lewicki

    发明人： Sarvajit Chakravarty ,  John J. Perumattam ,  George F. Schreiner ,  David Y. Liu ,  John A. Lewicki

    IPC分类号： A01N5500

    CPC分类号： C07D401/12 ,  A61K31/519 ,  C07D239/94 ,  C07D471/04

    摘要： The invention describes compounds of the formula and the pharmaceutically acceptable salts thereof and the pharmaceutically acceptable salts thereof wherein each R2 is independently a noninterfering substituent; m is an integer of 0-4; Z is CH or N; R1 is H, alkyl (1-6C) or arylalkyl optionally substituted on the aryl group with 1-3 substituents independently selected from alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, —SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C); n is 0, 1 or 2; Ar is phenyl, pyridyl, indolyl, or pyrimidyl, each optionally substituted with a group selected from the group consisting of optionally substituted alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C); and R3 is a branched or cyclic alkyl group (5-7C) or is phenyl optionally substituted with 1-2 substituents which substituents are selected from the group consisting of alkyl (1-6C), halo, OR, NR2, SR, —OOCR, —NROCR, RCO, —COOR, —CONR2, —SO2NR2, CN, CF3, and NO2, wherein each R is independently H or lower alkyl (1-4C) which are useful as antiinflammatories and in treating cardiac disorders.

    摘要翻译： 本发明描述了下式的化合物及其药学上可接受的盐及其药学上可接受的盐，其中R2各自独立地为非干扰性取代基; m为0-4的整数; Z为CH或N; R 1为H，烷基（1-6C） （1-6C），卤素，OR，NR2，SR，-OOCR，-NROCR，RCO，-COOR，-CONR2，-SO2NR2，CN等的任选取代的芳基， CF 3和NO 2，其中每个R独立地为H或低级烷基（1-4C）; n为0,1或2; Ar为苯基，吡啶基，吲哚基或嘧啶基，各自任选被选自以下的基团取代： 任选取代的烷基（1-6C），卤素，OR，NR2，SR，-OOCR，-NROCR，RCO，-COOR，-CONR2，SO2NR2，CN，CF3和NO2，其中每个R独立地为H或低级烷基 （1-4C）; 和R 3是支链或环状烷基（5-7C），或是任选被1-2个取代基取代的苯基，所述取代基选自烷基（1-6C），卤素，OR，NR2，SR，-OOCR， -NROCR，RCO，-COOR，-CONR2，-SO2NR2，CN，CF3和NO2，其中每个R独立地为H或可用作抗炎剂和治疗心脏疾病的低级烷基（1-4C）。