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    Quinazoline derivatives as medicaments
    21.
    发明申请
    Quinazoline derivatives as medicaments 有权
    喹唑啉衍生物作为药物

    公开(公告)号：US20050096333A1

    公开(公告)日：2005-05-05

    申请号：US10957183

    申请日：2004-09-30

    Applicant: Sundeep Dugar ,  Sarvajit Chakravarty ,  Alison Murphy ,  Glenn McEnroe ,  Aurelia Conte ,  John Perumattam

    Inventor： Sundeep Dugar ,  Sarvajit Chakravarty ,  Alison Murphy ,  Glenn McEnroe ,  Aurelia Conte ,  John Perumattam

    IPC: A61K20060101 ,  A61K31/4965 ,  A61K31/517 ,  A61K31/519 ,  C07D471/04 ,  C07D475/10 ,  C07D487/04

    CPC classification number: C07D471/04 ,  C07D475/10 ,  C07D487/04

    Abstract: Quinazoline derivatives have the formula: or the pharmaceutically acceptable salts thereof; wherein each of Z5, Z6, Z7 and Z8 is N or CH and wherein one or two Z5, Z6, Z7 and Z8 are N and wherein two adjacent Z positions cannot be N; wherein m and n are each independently 0-3; wherein R1 is independently OH, SH, NH2, OR, SR, NHR, halo or R-halide; wherein two adjacent R1 groups may be joined to form an aliphatic hetero cycle ring of 5-6 members; wherein R2 is independently R, halo, R-halide, OR-halide, NH2, CONH2 or CONHR; wherein R is optionally substituted C1-C12 alkyl, C1-C12 alkenyl, C1-C12 alkynyl, or aryl C1-C12 alkyl, containing 0-4 heteroatoms in place of a carbon in the carbon backbone, where the optional substituents are ═O, ═N, or OH; and wherein R3 is H or CH3. Such compounds are useful in pharmaceutical compositions and methods of treating conditions characterized by enhanced TGFβ activity.

    Abstract translation: 喹唑啉衍生物具有下式：或其药学上可接受的盐; 其中Z 5，Z 6，Z 7和Z 8各自为N或CH，其中一个或多个 两个Z 5，Z 6，Z 7和Z 8是N，并且其中两个相邻的Z位置不能是 N; 其中m和n各自独立地为0-3; 其中R 1独立地是OH，SH，NH 2，OR，SR，NHR，卤素或R卤化物; 其中两个相邻的R 1个基团可以连接形成5-6个成员的脂肪族杂环; 其中R 2独立地是R 1，R 2，R 2卤素，OR-卤素，NH 2，CONH 2或CONHR; 其中R是任选取代的C 1 -C 12烷基，C 1 -C 12 - 烯基，C

    Quinazoline derivatives as medicaments
    22.
    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

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

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

    IPC: C07D23942

    CPC classification number: C07D401/12 ,  A61K31/519 ,  C07D239/94 ,  C07D471/04

    Abstract: 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.

    Abstract translation: 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;
    23.
    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

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

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

    IPC: A01N5500

    CPC classification number: C07D401/12 ,  A61K31/519 ,  C07D239/94 ,  C07D471/04

    Abstract: 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.

    Abstract translation: 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）。

    Pyrido[4,3-b]indoles containing rigid moieties
    25.
    发明授权
    Pyrido[4,3-b]indoles containing rigid moieties 有权
    含有刚性部分的吡啶并[4,3-b]吲哚

    公开(公告)号：US08907097B2

    公开(公告)日：2014-12-09

    申请号：US12610217

    申请日：2009-10-30

    Applicant: David T. Hung ,  Andrew Asher Protter ,  Rajendra Parasmal Jain ,  Sarvajit Chakravarty

    Inventor： David T. Hung ,  Andrew Asher Protter ,  Rajendra Parasmal Jain ,  Sarvajit Chakravarty

    IPC: C07D401/00 ,  A61K31/445 ,  C07D401/14 ,  C07D471/04

    CPC classification number: C07D471/04 ,  C07D401/14

    Abstract: This disclosure is directed to pyrido[4,3-b]indoles having rigid moieties. The compounds in one embodiment are pyrido[4,3-b]indoles having an unsaturated hydrocarbon moiety. The compounds in another embodiment are pyrido[4,3-b]indoles having a cycloalkyl, cycloalkenyl or heterocyclyl moiety. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

    Abstract translation: 本公开涉及具有刚性部分的吡啶并[4,3-b]吲哚。 一个实施方案中的化合物是具有不饱和烃部分的吡啶并[4,3-b]吲哚。 另一个实施方案中的化合物是具有环烷基，环烯基或杂环基部分的吡啶并[4,3-b]吲哚。 还提供了包含化合物的药物组合物，以及在多种治疗应用中使用化合物的方法，包括治疗认知障碍，精神病性障碍，神经递质介导的病症和/或神经元病症。

    PYRIDO[4,3-B]INDOLES CONTAINING RIGID MOIETIES
    27.
    发明申请
    PYRIDO[4,3-B]INDOLES CONTAINING RIGID MOIETIES 有权
    PYRIDO [4,3-B]包含刚果的动物

    公开(公告)号：US20100216814A1

    公开(公告)日：2010-08-26

    申请号：US12610217

    申请日：2009-10-30

    Applicant: David T. HUNG ,  Andrew Asher Protter ,  Rajendra Parasmal Jain ,  Sarvajit Chakravarty

    Inventor： David T. HUNG ,  Andrew Asher Protter ,  Rajendra Parasmal Jain ,  Sarvajit Chakravarty

    IPC: A61K31/497 ,  C07D471/04 ,  A61K31/437 ,  C07D401/14 ,  A61K31/506 ,  A61P25/00

    CPC classification number: C07D471/04 ,  C07D401/14

    Abstract: This disclosure is directed to pyrido[4,3-b]indoles having rigid moieties. The compounds in one embodiment are pyrido[4,3-b]indoles having an unsaturated hydrocarbon moiety. The compounds in another embodiment are pyrido[4,3-b]indoles having a cycloalkyl, cycloalkenyl or heterocyclyl moiety. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.

    Abstract translation: 本公开涉及具有刚性部分的吡啶并[4,3-b]吲哚。 一个实施方案中的化合物是具有不饱和烃部分的吡啶并[4,3-b]吲哚。 另一个实施方案中的化合物是具有环烷基，环烯基或杂环基部分的吡啶并[4,3-b]吲哚。 还提供了包含化合物的药物组合物，以及在多种治疗应用中使用化合物的方法，包括治疗认知障碍，精神病性障碍，神经递质介导的病症和/或神经元病症。

    INDOLE-TYPE DERIVATIVES AS INHIBITORS OF p38 KINASE
    30.
    发明申请
    INDOLE-TYPE DERIVATIVES AS INHIBITORS OF p38 KINASE 审中-公开
    作为p38激酶的抑制剂的吲哚型衍生物

    公开(公告)号：US20070161649A1

    公开(公告)日：2007-07-12

    申请号：US11689418

    申请日：2007-03-21

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

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

    IPC: A61K31/496 ,  A61K31/454 ,  C07D403/02

    CPC classification number: C07D209/24 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

    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; 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是CA或CR 8 A，另一个是CR 1，CR 1，2， 其中每个R 1，R 6和R 8独立为氢，NR 6，N 6， 或非干扰取代基; A是其中Y是COR 2或其等同体和R 2的-Wi-i-X 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是NR 7或O; 每个R 3独立地是非干扰取代基; n为0-3; L 1和L 2各自为连接体; 每个R 4独立地是非干扰取代基; 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中的每一个是0-2的整数，其中1和k之和为0-3; Ar是被0-5个非直链取代基取代的芳基，其中两个非干扰取代基可以形成稠环; 并且与L 2连接的Ar原子和α环的中心之间的距离为4.5-24埃。

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