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    Indole-type derivatives as inhibitors of p38 kinase
    71.
    发明授权
    Indole-type derivatives as inhibitors of p38 kinase 有权
    吲哚型衍生物作为p38激酶的抑制剂

    公开(公告)号：US06867209B1

    公开(公告)日：2005-03-15

    申请号：US09575060

    申请日：2000-05-19

    Applicant: Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

    Inventor： Babu J. Mavunkel ,  Sarvajit Chakravarty ,  John J. Perumattam ,  Sundeep Dugar ,  Qing Lu ,  Xi Liang

    IPC: C07D209/08 ,  C07D209/24 ,  C07D235/06 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D471/04 ,  A61K31/495 ,  C07D241/04

    CPC classification number: C07D235/06 ,  C07D209/08 ,  C07D209/24 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D471/04

    Abstract: The invention is directed to methods to inhibit p38-α kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein represents a single or double bond; one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent; A is —Wi—COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2-6 Å, and each of i and j is independently 0 or 1; as Z3 is NR7 or O; each R3 is independently a noninterfering substituent; n is 0-3; each of L1 and L2 is a linker; each R4 is independently a noninterfering substituent; m is 0-4; Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent; each of 1 and k is an integer from 0-2 wherein the sum of 1 and k is 0-3; Ar is an aryl group substituted with 0-5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; and the distance between the atom of Ar linked to L2 and the center of the α ring is 4.5-24 Å.

    Abstract translation: 本发明涉及使用下式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激酶的方法，其中表示单键或双键;一个Z 2为CA或CR <8> A，另一个为CR <1> ，CR 1，NR 6或N，其中每个R 1，R 6和R 8独立地是氢或非干扰取代基; A是-Wi-COX j Y，其中Y是COR 2或 其等同基团和R 2是氢或非干扰取代基，W和X各自为2-6的间隔基，i和j各自独立地为0或1; Z 3为NR 7 >或O;每个R 3独立地为非干扰取代基; n为0-3; L 1和L 2各自为连接基;每个R 4独立地为非干扰取代基; m为0 -4; Z 1是CR 5或N，其中R 5是氢或非干扰取代基; 1和k各自是整数fr om 0-2其中1和k的和为0-3; Ar是被0-5个非干扰取代基取代的芳基，其中两个非干扰取代基可以形成稠环; 并且连接到L 2的Ar原子与α环的中心之间的距离为4.5-24。

    Bicyclic acyl guanidine sodium/proton exchange inhibitors and method
    74.
    发明授权
    Bicyclic acyl guanidine sodium/proton exchange inhibitors and method 有权
    双环酰基胍胍/质子交换抑制剂及方法

    公开(公告)号：US06630506B1

    公开(公告)日：2003-10-07

    申请号：US09556739

    申请日：2000-04-21

    Applicant: Sundeep Dugar ,  Steven V. O'Neil

    Inventor： Sundeep Dugar ,  Steven V. O'Neil

    IPC: C07D21554

    CPC classification number: C07D335/06 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D311/58 ,  C07D311/70 ,  C07D313/08 ,  C07D413/04 ,  C07D417/04

    Abstract: Acyl guanidines are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 0 to 4; X is a bond, O, S, SO, SO2, CO, or NR7; Y is a bond, O, S, SO, SO2, CO, or NR7′ wherein at least one of X and Y is other than a bond; and R1, R2, R3, R4, R5, R6, R7 and Ra, Rb, Rc, Rd are as defined herein, and are useful as antianginal, cardioprotective agents, antiischemic agents, and agents for peripheral vascular disease including intermittent claudication. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, arrhythmia, peripheral vascular diseases (PVD), including peripheral atherosclerotic disease (PAD), including intermittent claudication, Raynaud's diseases, and LeRiches Syndrome, pain, parethesia or discomfort in the lower limb and gluteal regions produced by vascular (e.g. arterial) insufficiency (where symptoms are initiated or worsened with ambulation), employing the above acyl guanidines.

    Abstract translation: 提供了酰基胍，其是具有n为0至4的结构的钠/质子交换（NHE）抑制剂; X是键，O，S，SO，SO 2，CO或NR 7; Y是键，O，S，SO，SO 2，CO或NR 7，其中X和Y中的至少一个不是键; R 1，R 2，R 3，R 4，R 5，R 6，R 7和R a，R b，R c， R d如本文所定义，并且可用作抗心绞痛，心脏保护剂，抗缺血剂和用于外周血管疾病（包括间歇性跛行）的药剂。 另外，提供了用于预防或治疗心绞痛，心功能不全，心肌坏死，心律失常，包括外周动脉粥样硬化性疾病（PAD）在内的外周血管病（PVD），包括间歇性跛行，雷诺氏病和莱氏综合征，疼痛， 使用上述酰基胍，由血管（例如动脉）不足（其中症状开始或恶化）产生的下肢和臀部区域的麻醉或不适感。

    Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
    75.
    再颁专利
    Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents 有权
    用作降胆固醇药的羟基取代的氮杂环丁酮化合物

    公开(公告)号：USRE37721E1

    公开(公告)日：2002-05-28

    申请号：US09594996

    申请日：2000-06-15

    Applicant: Stuart B. Rosenblum ,  Sundeep Dugar ,  Duane A. Burnett ,  John W. Clader ,  Brian A. McKittrick

    Inventor： Stuart B. Rosenblum ,  Sundeep Dugar ,  Duane A. Burnett ,  John W. Clader ,  Brian A. McKittrick

    IPC: C07D20508

    CPC classification number: C07D205/08 ,  A61K9/2018 ,  A61K9/4858 ,  A61K31/21 ,  A61K31/35 ,  A61K31/395 ,  A61K31/40 ,  A61K45/06 ,  Y02P20/55 ,  Y10S514/824 ,  A61K2300/00

    Abstract: Hydroxy-substituted azetidinone hypocholesterolemic agents of the formula or a pharmaceutically acceptable salt thereof, wherein: Ar1 and Ar2 are aryl or R4-substituted aryl; Ar3 is aryl or R5-substituted aryl; X, Y and Z are —CH2—, —CH(lower alkyl)— or —C(dilower alkyl)—; R and R2 are —OR6, —O(CO)R6, —O(CO)OR9 or —O(CO)NR6R7; R1 and R3 are H or lower alkyl; q is 0 or 1; r is 0 or 1; m, n and p are 0-4; provided that at least one of q and r is 1, and the sum of m, n, p, q and r is 1-6; and provided that when p is O and r is 1, the sum of m, q and n is 1-5; R4 is selected from lower alkyl, R5, —CF3, —CN, —NO2 and halogen R5 is selected from —OR6, —O(CO)R6, —O(CO)OR9, —O(CH2)1-5OR6, —O(CO)NR6R7, —NR6R7, —NR6(CO)R7, —NR6(CO)OR9, —NR6(CO)NR7R8, —NR6SO2R9, —COOR6, —CONR6R7, —COR6, —SO2NR6R7, S(O)0-2R9, —O(CH2)1-10—COOR6, —O(CH2)1-10CONR6R7, —(lower alkylene)COOR6 and —CH═CH—COOR6; R6, R7 and R8 are H, lower alkyl or aryl-substituted Ic R9 is lower alkyl, aryl or aryl-substituted lower alkyl; are disclosed, as well as a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor, pharmaceutical compositions containing them; and a process for preparing them.

    Abstract translation: 羟基取代的氮杂环丁酮低胆固醇血症药或其药学上可接受的盐，其中：Ar1和Ar2是芳基或R4取代的芳基; Ar3是芳基或R5-取代的芳基; X，Y和Z是-CH2-，-CH（ 低级烷基） - 或-C（二卤代烷基） - ; R和R 2为-OR 6，-O（CO）R 6，-O（CO）OR 9或-O（CO）NR 6 R 7; R 1和R 3为H或低级烷基; q为0或1; r为0或1; m，n和p为0-4; 条件是q和r中的至少一个为1，m，n，p，q和r的和为1-6; 并且条件是当p为O且r为1时，m，q和n的和为1-5; R 4选自低级烷基，R 5，-CF 3，-CN，-NO 2，卤素R 5选自-OR 6 ，-O（CO）R 6，-O（CO）OR 9，-O（CH 2）1-5 OR 6，-O（CO）NR 6 R 7，-NR 6 R 7，-NR 6（CO）R 7，-NR 6（CO）OR 9，-NR 6 （CO）NR7R8，-NR6SO2R9，-COOR6，-CONR6R7，-COR6，-SO2NR6R7，S（O）0-2R9，-O（CH2）1-10-COOR6，-O（CH2）1-10CONR6R7， - （ 低级亚烷基）COOR 6和-CH = CH-COOR 6; R6，R7和R8是H，低级烷基或芳基取代的IcR9是低级烷基，芳基或芳基取代的低级烷基;以及降低血清的方法 通过单独或与胆固醇生物合成抑制剂组合施用所述化合物，含有它们的药物组合物; 和一个准备它们的过程。

    Ether muscarinic antagonists
    78.
    发明授权
    Ether muscarinic antagonists 失效
    醚类毒蕈碱拮抗剂

    公开(公告)号：US5977138A

    公开(公告)日：1999-11-02

    申请号：US910616

    申请日：1997-08-13

    Applicant: Yuguang Wang ,  Wei K. Chang ,  Sundeep Dugar ,  Samuel Chackalamannil

    Inventor： Yuguang Wang ,  Wei K. Chang ,  Sundeep Dugar ,  Samuel Chackalamannil

    IPC: A61K45/06 ,  C07D211/46 ,  C07D211/96 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  A61K31/445 ,  C07D401/04

    CPC classification number: C07D405/12 ,  A61K45/06 ,  C07D211/46 ,  C07D211/96 ,  C07D405/14 ,  C07D409/14

    Abstract: 1,4 Di-substituted piperidine muscarinic antagonists of formula I ##STR1## or an isomer, pharmaceutically acceptable salt, ester or solvate thereof, whereinX is a bond, --O--, --S--, --SO--, --SO.sub.2 --, --CO--, --C(OR.sup.7).sub.2 --, --CH.sub.2 --O--, --O-- CH.sub.2 --, --CH.dbd.CH--, --CH.sub.2 --, --CH(C.sub.1 -C.sub.6 alkyl)-, --C(C.sub.1 -C.sub.6 alkyl).sub.2 --, --CONR.sup.17 --, --NR.sup.17 CO--, --O--C(O)NR.sup.17 --, --NR.sup.17 C(O)--O--, --SO.sub.2 NR.sup.17 -- or --NR.sup.17 SO.sub.2 --;R is cycloalkyl, optionally substituted phenyl or optionally substituted pyridyl;R.sup.2 is H, alkyl, optionally substituted cycloalkyl, cycloalkenyl, t-butoxycarbonyl or optionally substituted piperidinyl; and the remaining variables are as defined in the specification, are disclosed. Compounds of formula I are useful for treating cognitive disorders such as Alzheimer's disease. Also disclosed are pharmaceutical compositions, methods of preparation and combinations of compounds of formula I with ACh'ase inhibitors.

    Abstract translation: 1,4-二取代的式I的哌啶毒蕈碱拮抗剂或其异构体，药学上可接受的盐，酯或溶剂化物，其中X是键，-O - ， - S - ， - SO - ， - SO 2 - ， - ，-C（OR 7）2 - ， - CH 2 -O - ， - CH 2 - ， - CH = CH - ， - CH 2 - ， - CH（C 1 -C 6烷基） - ， - CONR 17 - ， - NR 17 CO - ， - OC（O）NR 17 - ， - NR 17 C（O）-O-，-SO 2 NR 17 - 或-NR 17 SO 2 - R是环烷基，任选取代的苯基或任选取代的吡啶基; R2是H，烷基，任选取代的环烷基，环烯基，叔丁氧羰基或任选取代的哌啶基; 并且其余变量如说明书中所定义。 式I化合物可用于治疗认知障碍如阿尔茨海默病。 还公开了药物组合物，制备方法和式I化合物与ACh酶抑制剂的组合。

    Spirocycloalkyl-substituted azetidinones useful as hypocholesterolemic agents
    80.
    发明授权
    Spirocycloalkyl-substituted azetidinones useful as hypocholesterolemic agents 失效
    螺环烷基取代的氮杂环丁酮可用作低胆固醇血症药

    公开(公告)号：US5698548A

    公开(公告)日：1997-12-16

    申请号：US449980

    申请日：1995-05-25

    Applicant: Sundeep Dugar ,  John W. Clader ,  Duane A. Burnett

    Inventor： Sundeep Dugar ,  John W. Clader ,  Duane A. Burnett

    IPC: A61K31/395 ,  A61K31/397 ,  A61K31/435 ,  A61K31/695 ,  A61P3/06 ,  A61P9/10 ,  C07D205/12 ,  C07D471/10 ,  C07F7/18 ,  C07D7/10

    CPC classification number: C07D471/10 ,  C07D205/12

    Abstract: Novel compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: R.sub.1 is ##STR2## R.sub.2 and R.sub.3 are independently selected from --CH.sub.2 --, --CH(lower alkyl)--, --C(di-lower alkyl)--, --CH.dbd.CH-- and --C(lower alkyl).dbd.CH--; or R.sub.1 with R.sub.2, or R.sub.1 with R.sub.3, form --CH.dbd.CH-- or --CH.dbd.C(lower alkyl)--; u and v are independently 0-3, provided both are not zero; R.sub.4 is B--(CH.sub.2).sub.m C(O)--; m is 0-5; B--(CH.sub.2).sub.q --; q is 0-6; B--(CH.sub.2).sub.e --Z--(CH.sub.2).sub.r ; Z is --O--, --C(O)--, phenylene, --N(R.sub.8)-- or --S(O).sub.0-2 --, e and r is 0-5; the sum of e and r is 0-6; B--(C.sub.2 -C.sub.6 alkenylene)--; B'--(C.sub.4 -C.sub.6 alkadienylene)--;B--(CH.sub.2).sub.t --Z--(C.sub.2 -C.sub.6 alkenylene)--; t is 0-3; the sum of t and the number of carbon atoms in the alkenylene chain is 2-6; B--(CH.sub.2).sub.f --V--(CH.sub.2).sub.g --; V is cycloalkylene, f is 1-5, g is 0-5; the sum of f and g is 1-6; B--(CH.sub.2).sub.t --V--(C.sub.2 -C.sub.6 alkenylene)-- or B'--(C.sub.2 -C.sub.6 alkenylene)--V--(CH.sub.2).sub.t --; the sum of t and the number of carbon atoms in the alkenylene chain is 2-6, B--(CH.sub.2).sub.a --Z--(CH.sub.2).sub.b --V--(CH.sub.2).sub.d --; a, b and d are 0-6; the sum of a, b and d is 0-6; T--(CH.sub.2).sub.s --; T is cycloalkyl, s is 0-6; or R.sub.1 and R.sub.4 together form ##STR3## B is optionally-substituted phenyl, indanyl, indenyl, naphthyl, tetrahydronaphthyl or optionally substituted-heteroaryl; and R.sub.20 and R.sub.21 are independently optionally-substituted phenyl, optionally-substituted naphthyl, indanyl, indenyl, tetrahydronaphthyl, benzodioxolyl, optionally-substituted heteroaryl, optionally-substituted benzofused heteroaryl or cyclopropyl, pharmaceutical compositions, the use as hypocholesterolemic agents, processes for preparing, and the use in combination with cholesterol biosynthesis inhibitors to treat or prevent athersclerosis.

    Abstract translation: 式（I）的新化合物或其药学上可接受的盐，其中：R 1是R 2和R 3独立地选自-CH 2 - ， - CH（低级烷基） - ， - C（二 - 低级 烷基） - ， - CH = CH-和-C（低级烷基）= CH-; 或R1与R2，或R1与R3形成-CH = CH-或-CH = C（低级烷基） - ; u和v独立为0-3，两者都不为零; R4是B-（CH2）mC（O） - ; m为0-5; B-（CH2）q-; q为0-6; B-（CH 2）e-Z-（CH 2）r; Z是-O - ， - C（O） - ，亚苯基，-N（R 8） - 或-S（O）0-2-，e和r是0-5; e和r的和为0-6; B-（C 2 -C 6亚烯基） - ; B' - （C 4 -C 6链二烯） - ; B-（CH 2）t-Z-（C 2 -C 6亚烯基） - ; t为0-3; 亚烯基链中t和碳原子数之和为2-6; B-（CH2）f-V-（CH2）g-; V是亚环烷基，f是1-5，g是0-5; f和g之和为1-6; B-（CH2）t-V-（C2-C6亚链烯基） - 或B' - （C2-C6亚烯基）-V-（CH2）t-; 亚烯基链中t和碳原子数之和为2-6，B-（CH2）a-Z-（CH2）b-V-（CH2）d-; a，b和d为0-6; a，b和d的和为0-6; T（CH 2）s - ; T是环烷基，s是0-6; 或R 1和R 4一起形成B是任选取代的苯基，茚满基，茚基，萘基，四氢萘基或任选取代的杂芳基; R20和R21独立地是任选取代的苯基，任选取代的萘基，茚满基，茚基，四氢萘基，苯并二恶唑基，任选取代的杂芳基，任选取代的苯并稠合的杂芳基或环丙基，药物组合物，用作低胆固醇血症药， 以及与胆固醇生物合成抑制剂组合用于治疗或预防硬化症的用途。

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