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80 条记录 (耗时 0.032 秒)

    Neuropeptide Y5 receptor antagonists
    52.
    发明授权
    Neuropeptide Y5 receptor antagonists 失效
    神经肽Y5受体拮抗剂

    公开(公告)号：US06329395B1

    公开(公告)日：2001-12-11

    申请号：US09326575

    申请日：1999-06-07

    申请人： Sundeep Dugar ,  Bernard R. Neustadt ,  Andrew W. Stamford ,  Yusheng Wu

    发明人： Sundeep Dugar ,  Bernard R. Neustadt ,  Andrew W. Stamford ,  Yusheng Wu

    IPC分类号： A61K31445

    CPC分类号： C07D213/40 ,  C07C233/15 ,  C07C233/25 ,  C07C233/29 ,  C07C275/28 ,  C07C275/32 ,  C07C275/34 ,  C07C275/38 ,  C07C311/05 ,  C07C323/41 ,  C07C323/44 ,  C07C2601/02 ,  C07C2601/08 ,  C07C2601/14 ,  C07D211/58 ,  C07D213/38 ,  C07D213/74 ,  C07D295/135 ,  C07D295/15 ,  C07D295/215 ,  C07D317/72

    摘要： Compounds of the formula I or a pharmaceutically acceptable salt thereof, wherein a and b are 0-2, provided that the sum is 0-3; X is —O—, —S—, —SO—, —SO2—, —CH(OR8)—, —C(O)—, —C(R23)2—, optionally substituted alkenyl, alkynyl or; R1 is optionally substituted aryl, heteroaryl, substituted amino, alkyl-OC(O)R8, aryloxyalkyl,  wherein m is 1-4, or  wherein d and e are 0-2; R2, R3, R4 and R5 are H, alkyl, optionally substituted cycloalkyl, halogen, —OR8, —N(R8)2, —CO2R8 or CF3; R6 and R7 are H, alkyl, alkenyl, hydroxyalkyl, aminoalkyl, alkoxy-alkyl, cycloalkyl or cycloalkylalkyl, or R6 and R7, form a 3-7-membered carbocyclic ring, or a 4-7-membered heterocyclic ring; R8 is H, alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R9 is alkyl, cycloalkyl, optionally substituted aryl or heteroaryl; R11 is H, alkyl or cycloalkyl; and R23 is R8 or halogen; are claimed, as well as additional novel compounds; also claimed are pharmaceutical compositions and methods of using said novel compounds in the treatment of eating disorders and diabetes.

    摘要翻译： 式I的化合物或其药学上可接受的盐，其中a和b为0-2，条件是总和为0-3; X是-O - ， - S - ， - SO - ， - SO 2 - ， - CH（OR 8 ） - ， - C（O） - ， - C（R 23）2 - ，任选取代的烯基，炔基或R 1是任选取代的芳基，杂芳基，取代的氨基，烷基-C（O）R 8，芳氧基烷基，其中m是1 -4或其中d和e为0-2; R 2，R 3，R 4和R 5为H，烷基，任选取代的环烷基，卤素，-OR 8，-N（R 8）2，-CO 2 R 8或CF 3; R 6和R 7为 H，烷基，烯基，羟基烷基，氨基烷基，烷氧基 - 烷基，环烷基或环烷基烷基，或R6和R7形成3-7元碳环或4-7元杂环; R8是H，烷基，环烷基 ，任选取代的芳基或杂芳基; R 9为烷基，环烷基，任选取代的芳基或杂芳基; R 11为H，烷基或环烷基; R 23为R 8或卤素; 以及其他新型化合物; 还要求的是使用所述新型化合物治疗进食障碍和糖尿病的药物组合物和方法。

    Quinazoline derivatives as medicaments
    53.
    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。

    Muscarinic antagonists
    55.
    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
    56.
    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
    57.
    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
    58.
    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。