利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

80 条记录 (耗时 0.042 秒)

    Muscarinic antagonists
    62.
    发明授权
    Muscarinic antagonists 失效
    毒蕈碱拮抗剂

    公开(公告)号：US5935958A

    公开(公告)日：1999-08-10

    申请号：US883183

    申请日：1997-06-26

    申请人： Joseph A. Kozlowski ,  Derek B. Lowe ,  Wei K. Chang ,  Sundeep Dugar

    发明人： Joseph A. Kozlowski ,  Derek B. Lowe ,  Wei K. Chang ,  Sundeep Dugar

    IPC分类号： C07D211/58 ,  C07D239/34 ,  C07D295/096 ,  C07D311/74 ,  A61K31/495 ,  A61K31/445 ,  C07D401/12 ,  C07D405/14

    CPC分类号： C07D295/096 ,  C07D211/58 ,  C07D239/34 ,  C07D311/74

    摘要： Di-N-substituted piperazine or 1,4-di-substituted piperidine compounds in accordance with formula I (including all isomers, salts, esters, and solvates) ##STR1## wherein Q, n, R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.21, R.sup.27, R.sup.28, X, and Z are as defined herein are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease. Pharmaceutical compositions and methods of preparation are also disclosed. Also disclosed are synergistic combinations with acetyl-cholinesterase inhibitors of compounds capable of enhancing acetylcholine release and having the above formula.

    摘要翻译： 根据式I的二-N-取代哌嗪或1,4-二取代哌啶化合物（包括所有异构体，盐，酯和溶剂化物）其中Q，n，R，R1，R2，R3，R4，R21， R27，R28，X和Z如本文所定义的是可用于治疗认知障碍如阿尔茨海默氏病的毒蕈碱拮抗剂。 还公开了药物组合物和制备方法。 还公开了与能够增强乙酰胆碱释放并具有上式的化合物的乙酰胆碱酯酶抑制剂的协同组合。

    Substituted .beta.-lactam compounds useful as hypochlesterolemic agents and processes for the preparation thereof
    63.
    发明授权
    Substituted .beta.-lactam compounds useful as hypochlesterolemic agents and processes for the preparation thereof 失效

    公开(公告)号：US5688787A

    公开(公告)日：1997-11-18

    申请号：US588785

    申请日：1996-01-19

    申请人： Duane A. Burnett ,  John W. Clader ,  Sundeep Dugar ,  Wayne Vaccaro

    发明人： Duane A. Burnett ,  John W. Clader ,  Sundeep Dugar ,  Wayne Vaccaro

    IPC分类号： C07D205/08 ,  C07D205/085 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07F7/08 ,  C07F7/18 ,  A61K31/395 ,  C07D403/10

    CPC分类号： C07D401/04 ,  C07D205/08 ,  C07D205/085 ,  C07D403/04 ,  C07D405/04 ,  C07D405/10 ,  C07D409/04 ,  C07F7/0812 ,  C07F7/186

    摘要： Novel compounds of the formula ##STR1## wherein A is --CH.dbd.CH--B; --C.tbd.C--B; --(CH.sub.2).sub.p --X--B, and X is a bone, --NH-- or --S(O).sub.0-2 --; optionally substituted heteroaryl or benzofused heteroaryl; --C(O)--B; or ##STR2## D is B'--(CH.sub.2).sub.m C(O)--, B'--(CH.sub.2).sub.q --, B'--(CH.sub.2).sub.e --Z--(CH.sub.2).sub.r, wherein Z is --O--, --C(O)--, phenylene, --NR.sub.8 -- or --S(O).sub.0-2 --, B'--(alkenylene)--; B'--(alkadienylene)--; B'--(CH.sub.2).sub.t --Z--(alkenylene), B'--(CH.sub.2).sub.f --V--(CH.sub.2).sub.g --, wherein V is cycloalkylene, B'--(CH.sub.2).sub.t --V--(alkenylene) or B'--(alkenylene)--V--(CH.sub.2).sub.t --, B'--(CH.sub.2).sub.a --Z--(CH.sub.2).sub.b --V--(CH.sub.2).sub.d --, T--(CH.sub.2).sub.s --, wherein T is cycloalkyl; naphthylmethyl or optionally substituted heteroarylmethyl; B is optionally substituted phenyl; B' is naphthyl, optionally substituted heteroaryl or optionally substituted phenyl; R is hydrogen, fluoro, alkyl, alkenyl, alkynyl, or B--(CH.sub.2).sub.n --; R.sub.4 is optionally substituted phenyl, indanyl, benzofuranyl, tetrahydronaphthyl, pyridyl, pyrazinyl, pyrimidinyl or quinolyl; are disclosed, the method of using compounds of the formula II ##STR3## wherein R.sub.20 is optionally substituted phenyl, naphthyl, heteroaryl, or benzofused heteroaryl, R.sub.21, R.sub.22 and R.sub.23 are H or R.sub.20 ; E, F and G are independently a bond; cycloalkylene; alkylene; alkenylene; alkynylene; a substituted alkylene, alkenylene or alkynylene chain; an interrupted alkylene, alkenylene or alkynylene chain; or an interrupted alkylene, alkenylene or alkynylene chain substituted by one or more substituents; or one of R.sub.21 --E and R.sub.22 --F is selected from the group consisting of halogeno, OH, alkoxy, --OC(O)R.sub.5, --NR.sub.10 R.sub.11, --SH or --S(alkyl); R.sub.5 is alkyl, phenyl, R.sub.14 -phenyl, benzyl or R.sub.14 -benzyl; R.sub.10 and R.sub.11 are independently selected from H and lower alkyl, or a pharmaceutically acceptable salt thereof, in a pharmaceutically aceptable carrier as hypocholesterolemic agents is also disclosed.

    Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents
    64.
    发明授权
    Sulfur-substituted azetidinone compounds useful as hypocholesterolemic agents 失效

    公开(公告)号：US5633246A

    公开(公告)日：1997-05-27

    申请号：US463619

    申请日：1995-06-05

    申请人： Brian A. McKittrick ,  Sundeep Dugar ,  Duane A. Burnett

    发明人： Brian A. McKittrick ,  Sundeep Dugar ,  Duane A. Burnett

    IPC分类号： A61K31/395 ,  A61K31/397 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/4433 ,  A61P3/06 ,  A61P9/10 ,  C07D205/08 ,  C07D401/12 ,  C07D409/12

    CPC分类号： C07D401/12 ,  C07D205/08 ,  C07D409/12

    摘要： Sulfur-substituted azetidinone hypocholesterolemic agents of the formula ##STR1## or a pharmaceutically acceptable salt thereof, wherein: Ar.sup.1 is aryl, R.sup.10 -substituted aryl or heteroaryl;Ar.sup.2 is aryl or R.sup.4 -substituted aryl;Ar.sup.3 is aryl or R.sup.5 -substituted aryl;X and Y are --CH.sub.2 --, --CH(lower alkyl)-- or --C(dilower alkyl)--;R is --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9 or --O(CO)NR.sup.6 R.sup.7 ; R.sup.1 is hydrogen, lower alkyl or aryl; or R and R.sup.1 together are .dbd.O;q is 0 or 1; r is 0, 1 or 2; m and n are 0-5; provided that the sum of m, n and q is 1-5;R.sup.4 is selected from lower alkyl, --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --(lower alkylene)--COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ;R.sup.5 is selected from --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --CF.sub.3, --CN, --NO.sub.2, halogen, --(lower alkylene)COOR.sup.6 and --CH.dbd.CH--COOR.sup.6 ;R.sup.6, R.sup.7 and R.sup.8 are H, lower alkyl, aryl or aryl-substituted lower alkyl;R.sup.9 is lower alkyl, aryl or aryl-substituted lower alkyl; andR.sup.10 is selected from lower alkyl, --OR.sup.6, --O(CO)R.sup.6, --O(CO)OR.sup.9, --O(CH.sub.2).sub.1-5 OR.sup.6, --O(CO)NR.sup.6 R.sup.7, --NR.sup.6 R.sup.7, --NR.sup.6 (CO)R.sup.7, --NR.sup.6 (CO)OR.sup.9, --NR.sup.6 (CO)NR.sup.7 R.sup.8, --NR.sup.6 SO.sub.2 R.sup.9, --COOR.sup.6, --CONR.sup.6 R.sup.7, --COR.sup.6, --SO.sub.2 NR.sup.6 R.sup.7, S(O).sub.0-2 R.sup.9, --O(CH.sub.2).sub.1-10 --COOR.sup.6, --O(CH.sub.2).sub.1-10 CONR.sup.6 R.sup.7, --CF.sub.3, --CN, --NO.sub.2 and halogen;are disclosed, as well as pharmaceutical compositions containing them, and a method of lowering serum cholesterol by administering said compounds, alone or in combination with a cholesterol biosynthesis inhibitor.

    1,2-disubstituted ethly amides as inhibitors of ACAT
    65.
    发明授权
    1,2-disubstituted ethly amides as inhibitors of ACAT 失效
    作为ACAT抑制剂的1,2-二取代的乙酰胺

    公开(公告)号：US5607931A

    公开(公告)日：1997-03-04

    申请号：US381958

    申请日：1995-03-20

    申请人： Sundeep Dugar

    发明人： Sundeep Dugar

    IPC分类号： C07D295/12 ,  A61K31/165 ,  A61K31/445 ,  A61K31/4468 ,  A61K31/495 ,  A61K31/535 ,  A61K31/5375 ,  A61P9/10 ,  A61P43/00 ,  C07C231/10 ,  C07C233/09 ,  C07D211/44 ,  C07D211/58 ,  C07D211/72 ,  C07D211/74 ,  C07D221/20 ,  C07D295/125 ,  C07D295/18 ,  C07D295/185 ,  C07D491/10 ,  C07D491/107 ,  C07D491/113

    CPC分类号： C07D221/20 ,  C07C233/09 ,  C07D211/44 ,  C07D211/58 ,  C07D211/72 ,  C07D211/74 ,  C07D295/125 ,  C07D295/185 ,  C07D491/10 ,  C07C2101/14

    摘要： Amides of the formula ##STR1## wherein: R.sup.1 is A and R.sup.2 is B; R.sup.1 is B and R.sup.2 is A; or R.sup.1 and R.sup.2 are independently selected from the group B;A is phenyl, substituted phenyl, heteroaryl, or substituted heteroaryl;B is cycloalkyl, substituted cycloalkyl, heterocycloalkyl, or substituted heterocycloalkyl;R.sup.3 is an alkyl chain of 1 to 25 carbon atoms, branched or straight; an alkenyl chain of 2 to 25 carbon atoms, branched or straight; a substituted alkyl chain; a substituted alkenyl chain; an interrupted alkyl chain; an interrupted alkenyl chain; a substituted interrupted alkyl chain; or a substituted interrupted alkenyl chain;R.sup.4 is hydrogen, lower alkyl, phenyl, Q-substituted phenyl, heteroaryl or Q-substituted heteroaryl;R.sup.6 and R.sup.7 are both H, or R.sup.6 and R.sup.7 together represent .dbd.O;or a pharmaceutically acceptable salt thereof;useful as inhibitors of acyl-coenzyme A:cholesterol acyl transferase and therefore in the treatment of atherosclerosis are disclosed.

    摘要翻译： PCT No.PCT / US93 / 08705 Sec。 371日期1995年3月20日 102（e）1995年3月20日PCT PCT 1993年9月21日PCT公布。 公开号WO94 / 06784 日期：1994年3月31日公式其中：R1为A，R2为B; R1为B，R2为A; 或R 1和R 2独立地选自B组; A是苯基，取代的苯基，杂芳基或取代的杂芳基; B是环烷基，取代的环烷基，杂环烷基或取代的杂环烷基; R3是1至25个碳原子的烷基链，分支或直链; 2至25个碳原子的链烯基，分支或直链; 取代的烷基链; 取代烯基链; 间断的烷基链; 中断的烯基链; 取代的中断的烷基链; 或取代的中断的烯基链; R4是氢，低级烷基，苯基，Q-取代的苯基，杂芳基或Q-取代的杂芳基; R6和R7均为H或R6，R7一起表示= O; 或其药学上可接受的盐; 可用作酰基辅酶A的抑制剂：胆固醇酰基转移酶，因此用于治疗动脉粥样硬化。

    Methods to synthesize indoles as precursors for pharmaceuticals
    69.
    发明申请
    Methods to synthesize indoles as precursors for pharmaceuticals 审中-公开
    合成吲哚作为药物前体的方法

    公开(公告)号：US20070066833A1

    公开(公告)日：2007-03-22

    申请号：US11507869

    申请日：2006-08-21

    申请人： Sundeep Dugar ,  Peter Giannousis

    发明人： Sundeep Dugar ,  Peter Giannousis

    IPC分类号： C07D209/04

    CPC分类号： C07D209/08

    摘要： The invention provides improved methods for the synthesis of indoles, especially useful for making indoles having an ester or amide group at C-5. The methods involve cyclization of a protected ortho-acetylene-substituted aniline derivative to produce an indole.

    摘要翻译： 本发明提供了用于合成吲哚的改进方法，特别可用于在C-5制备具有酯或酰胺基团的吲哚。 所述方法包括环化受保护的邻乙炔取代的苯胺衍生物以产生吲哚。