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    Cyclic bradykinin antagonist peptides
    61.
    发明授权
    Cyclic bradykinin antagonist peptides 失效
    循环缓激肽拮抗剂肽

    公开(公告)号：US5543496A

    公开(公告)日：1996-08-06

    申请号：US279763

    申请日：1994-07-25

    Applicant: Donald J. Kyle ,  Sarvajit Chakravarty

    Inventor： Donald J. Kyle ,  Sarvajit Chakravarty

    IPC: A61K38/00 ,  C07K7/18 ,  A61K38/12 ,  C07K7/52

    CPC classification number: C07K7/18 ,  A61K38/00 ,  Y10S930/27

    Abstract: Cyclic compounds based on a modified bradykinin sequence are potent bradykinin receptor antagonists. Amino acid substitutions are made at postions 2 and 5 or 6 to facilitate the cyclization of the peptide through covalent bonding of the amino acid side chains.The analogs produced are useful in treating conditions and diseases of a mammal and human in which an excess of bradykinin or related kinins are produced or injected such as by insect bites.

    Abstract translation: 基于修饰的缓激肽序列的环化合物是有效的缓激肽受体拮抗剂。 在位置2和5或6处进行氨基酸取代，以通过氨基酸侧链的共价键来促进肽的环化。 所产生的类似物可用于治疗其中产生或注射过量的缓激肽或相关激肽的哺乳动物和人的病症和疾病，例如通过昆虫叮咬。

    Pyrido-pyrimidine compounds as medicaments
    64.
    发明授权
    Pyrido-pyrimidine compounds as medicaments 有权
    吡啶 - 嘧啶化合物作为药物

    公开(公告)号：US07345045B2

    公开(公告)日：2008-03-18

    申请号：US11053121

    申请日：2005-02-07

    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: A61K31/4375 ,  C07D471/04

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

    Abstract: The invention is directed to methods to inhibit TGF-β and/or p38-α 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R 3是非干扰性取代基; 每个Z是CR 2或N，其中环A中不超过两个Z位是N，并且其中环A中的两个相邻Z位不能是N; 每个R 2独立地是非干扰取代基; L是连接体; n为0或1; 并且Ar'是任选被1-3个非干扰取代基取代的环脂族，环状杂脂族，芳族或杂芳族部分的残基。

    Quinazoline derivatives as medicaments
    65.
    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：US07232824B2

    公开(公告)日：2007-06-19

    申请号：US10957183

    申请日：2004-09-30

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

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

    IPC: C07D239/94 ,  C07D471/04

    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，并且其中一个或多个 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
    67.
    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：US06476031B1

    公开(公告)日：2002-11-05

    申请号：US09383825

    申请日：1999-08-27

    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: C07D23994

    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。

    PYRIDO[3,4-B]INDOLES AND METHODS OF USE
    69.
    发明申请
    PYRIDO[3,4-B]INDOLES AND METHODS OF USE 审中-公开

    公开(公告)号：US20130137705A1

    公开(公告)日：2013-05-30

    申请号：US13498099

    申请日：2010-09-23

    Applicant: Sarvajit Chakravarty

    Inventor： Rajendra Parasmal Jain ,  Sarvajit Chakravarty

    IPC: C07D471/04

    CPC classification number: C07D471/04

    Abstract: This disclosure relates to new heterocyclic compounds that may be used to modulate a histamine receptor in an individual. Pyrido[3,4-b]indoles are described, as are pharmaceutical compositions comprising the compounds and 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.

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