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21 条记录 (耗时 0.031 秒)

    Compounds and methods to treat cardiac failure and other disorders
    3.
    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
    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：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
    5.
    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。

    Pseudopeptide bradykinin receptor antagonists
    9.
    发明授权
    Pseudopeptide bradykinin receptor antagonists 失效
    伪肽缓激肽受体拮抗剂

    公开(公告)号：US5521158A

    公开(公告)日：1996-05-28

    申请号：US957879

    申请日：1992-10-08

    申请人： Donald J. Kyle ,  Babu J. Mavunkel

    发明人： Donald J. Kyle ,  Babu J. Mavunkel

    IPC分类号： A61K38/00 ,  C07K7/18 ,  A61K38/08

    CPC分类号： C07K7/18 ,  A61K38/00

    摘要： The invention relates to peptides of up to 10 amino acids that are synthesized by substituting at least one of the bradykinin amino acids found in positions 2, 3, 4 and 5 of the bradykinin peptide with a fatty acid amine. The modified bradykinin peptides produced confer increased resistance to enzymatic degradation and/or tissue specificity. The invention also relates to pharmaceutical preparations and processes of treatments using the modified bradykinin peptides.

    摘要翻译： 本发明涉及通过用脂肪酸胺代替缓激肽肽​​的2,3,4和5位中的至少一种缓激肽氨基酸来合成多达10个氨基酸的肽。 产生的修饰的缓激肽多肽对酶降解和/或组织特异性的抗性增加。 本发明还涉及使用改良的缓激肽肽的药物制剂和治疗方法。

    Oximes of oxymorphone, naltrexone and naloxone as potent, selective opioid receptor agonists and antagonists
    10.
    发明授权
    Oximes of oxymorphone, naltrexone and naloxone as potent, selective opioid receptor agonists and antagonists 失效
    羟吗啡酮，纳曲酮和纳洛酮作为有效的选择性阿片受体激动剂和拮抗剂

    公开(公告)号：US4889860A

    公开(公告)日：1989-12-26

    申请号：US35034

    申请日：1987-04-06

    申请人： Waclaw J. Rzeszotarski ,  Babu J. Mavunkel

    发明人： Waclaw J. Rzeszotarski ,  Babu J. Mavunkel

    IPC分类号： C07D489/08

    CPC分类号： C07D489/08

    摘要： A potent, selective opioid receptor agonist or antagonist exhibiting properties useful for a longacting analgesic or opiate abuse treatment agent or appetite suppressant having the general formula: ##STR1## wherein R is methyl, cyclopropylmethyl or allyl, and R.sub.1 is an unsubstituted or substituted aryl, aralkyl, heteroaryl, heteroaralkyl or a cycloalkyl group with or without a heteroatom like S,O,N; and the pharmaceutically acceptable salts thereof.

    摘要翻译： 一种有效的选择性阿片样物质受体激动剂或拮抗剂，其具有用于具有以下通式的长效止痛剂或阿片剂滥用治疗剂或食欲抑制剂的性质：其中R为甲基，环丙基甲基或烯丙基，R 1为未取代或取代的芳基， 芳烷基，杂芳基，杂芳烷基或具有或不具有杂原子如S，O，N的环烷基; 及其药学上可接受的盐。