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    COMPOSITIONS AND METHODS FOR TREATING RESPIRATORY DISORDERS
    31.
    发明申请
    COMPOSITIONS AND METHODS FOR TREATING RESPIRATORY DISORDERS 审中-公开
    用于治疗呼吸障碍的组合物和方法

    公开(公告)号：WO2007103970A2

    公开(公告)日：2007-09-13

    申请号：PCT/US2007063479

    申请日：2007-03-07

    Applicant: ENDACEA INC ,  WILSON CONSTANCE N ,  PARTRIDGE JOHN J

    Inventor： WILSON CONSTANCE N ,  PARTRIDGE JOHN J

    IPC: C07D473/04 ,  A61K31/52 ,  A61P11/00

    CPC classification number: C07D473/04 ,  A61K31/522 ,  C07D473/06

    Abstract: Methods and compositions for treating and preventing respiratory disorders are provided. The methods of the invention comprise administering to a subject a therapeutically effective amount of a pharmaceutically acceptable salt of an A 1 adenosine receptor antagonist, particularly l-hydroxy-2-naphthoic acid salts or 3- hydroxy -2-naphthoic acid salts, more particularly a l-hydroxy-2-naphthoic acid salt of 3-[2-(4-aminophenyl)ethyl]-8-benzyl-7-{2-[ethyl-(2-hydroxyethyl)amino]ethyl}-l- propyl-3,7-dihydropurine-2,6-dione (i.e., an L-97-1 xinafoic acid salt). Hydrates of the A 1 adenosine receptor antagonist salts described herein are further provided. The invention further encompasses pharmaceutical compositions comprising a pharmaceutically acceptable salt of an A 1 adenosine receptor antagonist in a pharmaceutically acceptable carrier. The compositions of the invention find use in methods for treating and preventing respiratory disorders.

    Abstract translation: 提供了治疗和预防呼吸系统疾病的方法和组合物。 本发明的方法包括向受试者施用治疗有效量的A 1 N 2腺苷受体拮抗剂的药学上可接受的盐，特别是1-羟基-2-萘甲酸盐或3-羟基-2 - 萘甲酸盐，更特别是3- [2-（4-氨基苯基）乙基] -8-苄基-7- {2- [乙基 - （2-羟乙基）氨基]乙酸的1-羟基-2-萘甲酸盐， 乙基} -1-丙基-3,7-二氢嘌呤-2,6-二酮（即L-97-1十一酸盐）。 进一步提供本文所述的A 1 N 2腺苷受体拮抗剂盐的水合物。 本发明还包括在药学上可接受的载体中包含A 1 N 2腺苷受体拮抗剂的药学上可接受的盐的药物组合物。 本发明的组合物可用于治疗和预防呼吸系统疾病的方法。

    METHODS AND COMPOSITIONS FOR PRODUCING ANTIGENIC RESPONSES
    32.
    发明申请
    METHODS AND COMPOSITIONS FOR PRODUCING ANTIGENIC RESPONSES 审中-公开

    公开(公告)号：WO2005026318A3

    公开(公告)日：2005-03-24

    申请号：PCT/US2004/024693

    申请日：2004-07-30

    Applicant: ENDACEA, INC. ,  WILSON, Constance, N. ,  BORRON, Paul

    Inventor： WILSON, Constance, N. ,  BORRON, Paul

    IPC: A61K39/00

    Abstract: The present invention relates to methods of producing an antigenic response in which an antigen is contacted to an antigen-presenting cell, wherein the improvement comprises contacting the antigen-presenting cell with an A1 adenosine receptor activating agent in an amount sufficient to increase the antigenic response of the antigen-presenting cell to the antigen. The present invention further provides methods, compositions, combination therapies, imaging techniques, and diagnostic kits that may improve the diagnosis, prognosis, and/or survival of cancer patients, pathogen-infected patients, and infectious or non-infectious immune-deficient patients.

    METHODS AND PHARMACEUTICAL COMPOSITIONS FOR PREVENTING AND TREATING RENAL IMPAIRMENT
    34.
    发明申请
    METHODS AND PHARMACEUTICAL COMPOSITIONS FOR PREVENTING AND TREATING RENAL IMPAIRMENT 审中-公开
    用于预防和治疗肾功能不全的方法和药物组合物

    公开(公告)号：WO2011094208A2

    公开(公告)日：2011-08-04

    申请号：PCT/US2011/022411

    申请日：2011-01-25

    Applicant: ENDACEA, INC. ,  WILSON, Constance, N.

    Inventor： WILSON, Constance, N.

    IPC: A61K31/52 ,  A61K31/519 ,  A61P13/12 ,  A61P13/00

    CPC classification number: A61K31/522 ,  A61K31/519 ,  A61K31/52 ,  A61K45/06

    Abstract: The present invention relates to methods for treating and preventing renal impairment by administering to a subject a therapeutically effective amount of an A 1 adenosine receptor antagonist alone or in combination with at least one additional therapeutic agent. The invention further encompasses pharmaceutical compositions comprising an A 1 adenosine receptor antagonist alone or with, at least, one additional therapeutic agent in a pharmaceutically acceptable carrier. The pharmaceutical compositions of the invention find use in methods for treating and preventing renal impairment.

    Abstract translation: 本发明涉及通过向受试者施用单独的或与至少一种其它治疗剂组合的治疗有效量的A1腺苷受体拮抗剂来治疗和预防肾损伤的方法。 本发明还包括药物组合物，其单独或与药学上可接受的载体中的至少一种另外的治疗剂一起包含A1腺苷受体拮抗剂。 本发明的药物组合物可用于治疗和预防肾损伤的方法。

    A1 ADENOSINE RECEPTOR ANTAGONISTS
    35.
    发明申请
    A1 ADENOSINE RECEPTOR ANTAGONISTS 审中-公开
    A1腺苷受体拮抗剂

    公开(公告)号：WO2009086077A2

    公开(公告)日：2009-07-09

    申请号：PCT/US2008087638

    申请日：2008-12-19

    Applicant: ENDACEA INC

    Inventor： WILSON CONSTANCE N

    IPC: C07D473/14

    CPC classification number: C07D473/06

    Abstract: This invention relates to compounds of formula (I), Wherein R1 - R4 are defined in the Specification, their uses in the practice of medicine, their medicinal formulations, their use in medical diagnosis, and their preparation.

    Abstract translation: 本发明涉及式（I）化合物，其中R1-R4在本说明书中定义，它们在医学实践中的用途，它们的药物制剂，它们在医学诊断中的应用及其制备。

    COMPOSITIONS AND METHODS FOR TREATING RESPIRATORY DISORDERS
    36.
    发明申请
    COMPOSITIONS AND METHODS FOR TREATING RESPIRATORY DISORDERS 审中-公开

    公开(公告)号：WO2007103970A3

    公开(公告)日：2007-09-13

    申请号：PCT/US2007/063479

    申请日：2007-03-07

    Applicant: ENDACEA, INC. ,  WILSON, Constance, N. ,  PARTRIDGE, John, J.

    Inventor： WILSON, Constance, N. ,  PARTRIDGE, John, J.

    IPC: C07D473/04 ,  A61K31/52 ,  A61P11/00

    Abstract: Methods and compositions for treating and preventing respiratory disorders are provided. The methods of the invention comprise administering to a subject a therapeutically effective amount of a pharmaceutically acceptable salt of an A 1 adenosine receptor antagonist, particularly 1-hydroxy-2-naphthoic acid salts or 3- hydroxy-2-naphthoic acid salts, more particularly a 1-hydroxy-2-naphthoic acid salt of 3-[2-(4-aminophenyl)ethyl]-8-benzyl-7- {2-[ethyl-(2-hydroxyethyl)amino]ethyl} - 1 propyl-3,7-dihydropurine-2,6-dione (i.e., an L-97-1 xinafoic acid salt). Hydrates of the A 1 adenosine receptor antagonist salts described herein are further provided. The invention further encompasses pharmaceutical compositions comprising a pharmaceutically acceptable salt of an A 1 adenosine receptor antagonist in a pharmaceutically acceptable carrier. The compositions of the invention find use in methods for treating and preventing respiratory disorders.

    A1 ADENOSINE RECEPTOR ANTAGONISTS
    39.
    发明申请
    A1 ADENOSINE RECEPTOR ANTAGONISTS 审中-公开
    A1腺苷受体拮抗剂

    公开(公告)号：WO2004110379A3

    公开(公告)日：2005-03-24

    申请号：PCT/US2004018171

    申请日：2004-06-07

    Applicant: ENDACEA INC ,  WILSON CONSTANCE N ,  PARTRIDGE JOHN J

    Inventor： WILSON CONSTANCE N ,  PARTRIDGE JOHN J

    IPC: A61K20060101 ,  A61K31/522 ,  A61P3/04 ,  A61P3/10 ,  A61P9/04 ,  A61P11/06 ,  A61P13/12 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  A61P29/00 ,  A61P37/08 ,  C07D473/06

    CPC classification number: C07D473/06

    Abstract: This invention relates to compounds of formula (I): wherein R1 is a branched or straight chain C1-C8 alkyl; R2 is of the formula (II), wherein n is an integer ranging from 1 to 8; R5 is H or (CH2)pCH3, and R6 is H or (CH2)mOH, wherein p is an integer ranging from 1 to 7 and m is an integer ranging from 1 to 8; R3 is of the formula (III), wherein q is an integer ranging from 1 to 8; and R7 is selected from the group consisting of H, OH, NH2, (CH2)tOH, and R9COOH; wherein R9 is a straight or branched chain alkylene or alkenylene group having 1 to 8 carbon atoms, and t is an integer ranging from 1 to 8; R4 is of the formula (IV), wherein r is an integer ranging from 1 to 8 and R8 is selected from the group consisting of H, OH, (CH2)fNH2, (CH2)sOH, and R10COOH; wherein f is 0 or f and s are independently integers ranging from 1 to 8; and, R10 is a C1-C8 straight or branched chain alkylene or alkenylene; and; salts, solvates, and hydrates thereof. The present invention further provides methods of preparing the compounds of formula (I) and their use as therapeutic agents and diagnostic agents.

    Abstract translation: 本发明涉及式（I）化合物：其中R1是支链或直链C1-C8烷基; R2为式（Ⅱ），其中n为1至8的整数; R5是H或（CH2）pCH3，R6是H或（CH2）mOH，其中p是1到7的整数，m是1到8的整数; R3是式（III），其中q是1至8的整数; 并且R 7选自H，OH，NH 2，（CH 2）t OH和R 9 COOH; 其中R9为碳原子数为1〜8的直链或支链亚烷基或亚链烯基，t为1〜8的整数。 R4为式（Ⅳ），其中r为1至8的整数，R8选自H，OH，（CH2）fNH2，（CH2）sOH和R10COOH; 其中f为0或f且s为独立地为1至8的整数; 且R10为C1-C8直链或支链亚烷基或亚烯基; 和; 盐，溶剂化物和水合物。 本发明还提供制备式（I）化合物及其作为治疗剂和诊断剂的用途的方法。

    A1 ADENOSINE RECEPTOR ANTOGONISTS
    40.
    发明申请
    A1 ADENOSINE RECEPTOR ANTOGONISTS 审中-公开
    A1腺苷受体拮抗剂

    公开(公告)号：WO2005009343A2

    公开(公告)日：2005-02-03

    申请号：PCT/US2004/018044

    申请日：2004-06-04

    Applicant: ENDACEA, INC. ,  WILSON, Constance, N. ,  PARTRIDGE, John, J.

    Inventor： WILSON, Constance, N. ,  PARTRIDGE, John, J.

    IPC: A61K

    CPC classification number: C07D473/04 ,  C07D473/06

    Abstract: This invention relates to compounds of formula (I): (insert formula I) wherein; R1 is C1-8 straight or branched alkyl optionally substituted with one or more OR5, NR6R7, or halogen groups, wherein; R5 and R6 are independently H, or C1-8 straight or branched alkyl; R7 is H, C1-8 straight or branched alkyl, or Alk1-OH, wherein; Alk1 is C1-8 straight or branched alkylene; R2 is H, C1-8 alkyl, Alk2COOH, Alk3COOR8, Alk4CONR9R10, Alk5OH, Alk6SO3H, Alk7PO3H2, Alk8OR11, Alk9OH or Alk10NR12R13, or, when R3 is (CH2)q(C6H4)Q, R2 is as defined above or is Alk11N(CH3)Alk12OH; and when R3 is other than (CH2)q(C6H4)Q, R2 is as defined above or is Alk13NR14R15; wherein; Alk2 through Alk13 are independently C1-8 straight or branched alkylene or alkenylene; q is an integer ranging from 1 to 8; Q is H, OH, NH2, (CH2)t OH, or R13aCOOH, wherein t is an integer ranging from 1 to 8; R8 through R13, and R13a are independently H, or C1-8 straight or branched alkyl; R14 is H, CH3, or (CH2)p1CH3; R15 is H, CH3, (CH2)p2CH3 or (CH2)mOH, wherein; p1 and p2 are independently integers from 1 to 7, and m is an integer from 1 to 8; R3 is Alk14ArR16, wherein; Alk14 is C1-8 straight or branched alkylene or alkenylene; Ar is a 5- or 6-member aromatic ring containing 0 to 4 heteroatoms selected from N, O, and S, or is a bicyclic 9- or 11-member aromatic ring containing 0 to 6 heteroatoms selected from N, O, and S; R16 is H, OH, OR13b, NO2, NH2, CN, Alk15OH, Alk16NH2, NR17R18, NR19COR19a, Alk17COOR19b, SO2R19c, SO3H, PO3H2 or halogen; wherein; Alk15 through Alk17 are independently C1-8 straight or branched alkylene or alkenylene; R13b is H, or C1-8 straight or branched alkyl; R17, through R19 and R19a through R19c are independently H, an aromatic group, or C1-8 straight or branched alkyl; R4 is (insert formula here) wherein; r is an integer from 1 to 20; R20 is SO3H, PO3H2, halogen, OR13c, COOR13d, NO2, NR21R22, NR23COR23a, Alk18COOR19d, SO2R19e or Alk18NR24R25 and when R3 is other than (CH2)q(C6H4)Q, R20 is as defined above or is H, OH, NH2 Alk19OH, Alk20NH2, or Alk21COOH; wherein; Alk19 through Alk21 are independently C1-8 straight or branched alkylene or alkenylene; R13c and R13d are independently C1-8 straight or branched alkyl; R19d and R19e are independently H, an aromatic group or C1-8 straight or branched alkyl; R21, through R25 and R23a are independently H, an aromatic group or C1-8 straight or branched alkyl; wherein the compound optionally has one or more radioactive or non-radioactive label moieties wherein the label moieties are optionally connected to the compound through one or more spacer moiety; and salts, solvates and hydrates thereof; and salts, solvates, and hydrates thereof. The present invention further provides for their use as therapeutic agents and diagnostic agents.

    Abstract translation: 本发明涉及式（I）化合物：（式Ⅰ）其中： R1是任选被一个或多个OR 5，NR 6 R 7或卤素基团取代的C 1-8直链或支链烷基，其中; R 5和R 6独立地为H或C 1-8直链或支链烷基; R7是H，C1-8直链或支链烷基或Alk1-OH，其中; Alk1是C1-8直链或支链亚烷基; R2是H，C1-8烷基，Alk2COOH，Alk3COOR8，Alk4CONR9R10，Alk5OH，Alk6SO3H，Alk7PO3H2，Alk8OR11，Alk9OH或Alk10NR12R13，或者当R3是（CH2）q（C6H4）Q时，R2如上所定义或是Alk11N CH3）Alk12OH; 当R 3不是（CH 2）q（C 6 H 4）Q时，R 2如上定义或是Alk 13 NR 14 R 15; 其中; Alk2至Alk13独立地为C1-8直链或支链亚烷基或亚烯基; q为1〜8的整数; Q是H，OH，NH 2，（CH 2）t OH或R 13 aCOOH，其中t是1至8的整数; R 8至R 13和R 13a独立地为H或C 1-8直链或支链烷基; R14是H，CH3或（CH2）p1CH3; R15是H，CH3，（CH2）p2CH3或（CH2）mOH，其中; p1和p2独立地为1至7的整数，m为1至8的整数; R3是Alk14ArR16，其中; Alk14是C1-8直链或支链亚烷基或亚烯基; Ar是含有0至4个选自N，O和S的杂原子的5或6元芳环，或是含有0至6个选自N，O和S的杂原子的双环9或11元芳环 ; R16是H，OH，OR13b，NO2，NH2，CN，Alk15OH，Alk16NH2，NR17R18，NR19COR19a，Alk17COOR19b，SO2R19c，SO3H，PO3H2或卤素; 其中; Alk15至Alk17独立地为C1-8直链或支链亚烷基或亚烯基; R13b是H或C1-8直链或支链烷基; R 17，R 19和R 19a至R 19c独立地为H，芳基或C 1-8直链或支链烷基; R4是（在此插入式）其中; r为1〜20的整数; R 20是SO 3 H，PO 3 H 2，卤素，OR 13 c，COOR 13d，NO 2，NR 21 R 22，NR 23 COR 23 a，Alk 18 COOR 19d，SO 2 R 19e或Alk 18 NR 24 R 25，当R 3不是（CH 2）q（C 6 H 4）Q时，R 20如上所定义或是H，OH， Alk19OH，Alk20NH2或Alk21COOH; 其中; Alk19至Alk21独立地为C1-8直链或支链亚烷基或亚烯基; R 13c和R 13d独立地为C 1-8直链或支链烷基; R 19d和R 19e独立地为H，芳基或C 1-8直链或支链烷基; R 21，R 25和R 23a独立地为H，芳基或C 1-8直链或支链烷基; 其中所述化合物任选地具有一个或多个放射性或非放射性标记部分，其中所述标记部分任选地通过一个或多个间隔子部分与所述化合物连接; 及其盐，溶剂化物和水合物; 及其盐，溶剂化物和水合物。 本发明进一步提供它们作为治疗剂和诊断剂的用途。

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