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    A1 ADENOSINE RECEPTOR ANTOGONISTS
    5.
    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：WO2005009343A3

    公开(公告)日：2005-05-12

    申请号：PCT/US2004018044

    申请日：2004-06-04

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

    Inventor： WILSON CONSTANCE N ,  PARTRIDGE JOHN J

    IPC: A61K20060101 ,  A61K31/522 ,  A61P9/04 ,  A61P11/00 ,  A61P11/06 ,  A61P25/16 ,  A61P25/24 ,  A61P25/28 ,  A61P31/18 ,  A61P37/06 ,  A61P37/08 ,  C07D473/02 ,  C07D473/04 ,  C07D473/06

    CPC classification number: C07D473/04 ,  C07D473/06

    Abstract: 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; R4 is --((CH2)r-Phenyl-R20 wherein r is 1 to 20, R20 is SO3H, PO3H2, halogen, OR13c, COOR13d, NO2, NR21R22, and other choices. 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. The present invention also provides for their use as therapeutic agents and diagnostic agents.

    Abstract translation: 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，或是双环9或11 含有0至6个选自N，O和S的杂原子的芳族环; R4是 - （（CH2）r-苯基-R20，其中r为1-20，R20为SO3H，PO3H2，卤素，OR13c，COOR13d，NO2，NR21R22等选择，化合物任选具有一个或多个放射性或非 - 放射性标记部分，其中标记部分任选地通过一个或多个间隔基部分与化合物连接。本发明还提供它们作为治疗剂和诊断剂的用途。

    COMPOSITIONS AND METHODS FOR TREATING RESPIRATORY DISORDERS
    6.
    发明专利
    COMPOSITIONS AND METHODS FOR TREATING RESPIRATORY DISORDERS 未知

    公开(公告)号：CA2644613A1

    公开(公告)日：2007-09-13

    申请号：CA2644613

    申请日：2007-03-07

    Applicant: ENDACEA INC

    Inventor： PARTRIDGE JOHN J ,  WILSON CONSTANCE N

    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
    7.
    发明专利
    A1 ADENOSINE RECEPTOR ANTAGONISTS 未知

    公开(公告)号：CA2528367A1

    公开(公告)日：2004-12-23

    申请号：CA2528367

    申请日：2004-06-07

    Applicant: ENDACEA INC

    Inventor： WILSON CONSTANCE N ,  PARTRIDGE JOHN J

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

    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; R 4 is of the formula (IV), wherein r is an integer ranging from 1 to 8 and R8 i s selected from the group consisting of H, OH, (CH2)fNH2, (CH2)sOH, and R10COO H; wherein f is 0 or f and s are independently integers ranging from 1 to 8; an d, R10 is a C1-C8 straight or branched chain alkylene or alkenylene; and; salts , solvates, and hydrates thereof. The present invention further provides metho ds of preparing the compounds of formula (I) and their use as therapeutic agent s and diagnostic agents.

    COMPOSITIONS AND METHODS FOR TREATING RESPIRATORY DISORDERS
    8.
    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。

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