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39 条记录 (耗时 0.058 秒)

    Adenosine A2a receptor antagonists
    8.
    发明授权
    Adenosine A2a receptor antagonists 有权
    腺苷A2a受体拮抗剂

    公开(公告)号：US07041666B2

    公开(公告)日：2006-05-09

    申请号：US10304504

    申请日：2002-11-26

    申请人： Julius J. Matasi ,  John P. Caldwell ,  Deen Tulshian ,  Lisa S. Silverman ,  Bernard R. Neustadt

    发明人： Julius J. Matasi ,  John P. Caldwell ,  Deen Tulshian ,  Lisa S. Silverman ,  Bernard R. Neustadt

    IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/18 ,  A61P25/16 ,  A61P25/28

    CPC分类号： C07D487/04

    摘要： Disclosed are compounds having the structural formula or pharmaceutically acceptable salts or solvates thereof, wherein R is optionally substituted heteroaryl, optionally substituted phenyl, cycloalkenyl, —C(═CH2)CH3, —C≡C—CH3, —CH═C(CH3)2, or —CH═CH—CH3; R2 is —W—X, —NR19(CH2)m—W—X, and —NR19CH(CH3)—W—X, or R2 is alkyl, alkenyl and —NR18R19, each optionally substituted —W—X; R3 is H, halo, alkyl, trifluoromethyl, alkoxy, alkoxyalkyl, hydroxyalkyl, alkylamino, alkylaminoalkyl, dialkylamino, dialkylaminoalkyl, aminoalkyl, aryl, heteroaryl, or CN; R18 is a bond, —CH(OH)—, —CH(CH3)—, —C(CH3)n—, —(CH2)n—or —O(CH2)n—; W is aryl or heteroaryl, each optionally substituted; X is H, NH2, or substituted amino, or X is —R18—Y-Z; and n, R19, Y and Z are as defined in the specification; pharmaceutical compositions thereof, and methods of treating stroke or central nervous system diseases by administering the compound of the present invention to a patient in need of such treatment.

    摘要翻译： 公开了具有结构式或其药学上可接受的盐或溶剂化物的化合物，其中R是任选取代的杂芳基，任选取代的苯基，环烯基，-C（-CH 2 CH 2）CH 3 ，-C≡C-CH 3，-CH-C（CH 3）2，或-CH-CH-CH 3 ; R 2是-WX，-NR 19（CH 2）2 -WX和-NR O SUP CH 3（CH 3 CH 3）-WX或R 2是烷基，烯基和-NR 18 R 12， 19，每个任选取代的-WX; R 3是H，卤素，烷基，三氟甲基，烷氧基，烷氧基烷基，羟基烷基，烷基氨基，烷基氨基烷基，二烷基氨基，二烷基氨基烷基，氨基烷基，芳基，杂芳基或CN; -CH（OH） - ， - CH（CH 3） - ， - （CH 3 CH 3） - ， - （CH 3 CH 3） n - - （CH 2）n - 或 - （CH 2）n - / > - ; W是芳基或杂芳基，各自任选被取代; X是H，NH 2或取代的氨基，或X是-R 18 -Y-Z; 和n，R 19，Y和Z如说明书中所定义; 其药物组合物，以及通过将本发明化合物给予需要这种治疗的患者来治疗中风或中枢神经系统疾病的方法。

    High affinity ligands for nociceptin receptor ORL-1
    9.
    发明授权
    High affinity ligands for nociceptin receptor ORL-1 有权
    伤害感受器受体ORL-1的高亲和力配体

    公开(公告)号：US06455527B2

    公开(公告)日：2002-09-24

    申请号：US09769824

    申请日：2001-01-25

    申请人： Deen Tulshian ,  Ginny D. Ho ,  Lisa S. Silverman ,  Julius J. Matasi ,  Robbie L. McLeod ,  John A. Hey ,  Richard W. Chapman ,  Ana Bercovici ,  Francis M. Cuss

    发明人： Deen Tulshian ,  Ginny D. Ho ,  Lisa S. Silverman ,  Julius J. Matasi ,  Robbie L. McLeod ,  John A. Hey ,  Richard W. Chapman ,  Ana Bercovici ,  Francis M. Cuss

    IPC分类号： A61K31445

    CPC分类号： A61K45/06 ,  A61K31/00 ,  A61K31/438 ,  A61K31/439 ,  A61K31/451 ,  A61K31/4535 ,  A61K31/454

    摘要： Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN ; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.

    摘要翻译： 式的新型化合物或其药学上可接受的盐或溶剂化物，其中：虚线表示任选的双键; X 1为任选取代的烷基，环烷基，芳基，杂芳基或杂环烷基; X 2为-CHO，-CN，任选取代的氨基， 烷基或芳基;或X 1是任选取代的苯并稠合的杂环基，并且X 2是氢;或者X 1和X 2一起形成任选的苯并稠合的螺杂环基R1，R2，R3和R4独立地是H和烷基，或（R1和R4）或 和（R 3和R 3）或（R 1和R 3）或（R 2和R 4）在一起可以形成1至3个碳原子的亚烷基桥; Z 1是任选取代的烷基，芳基，杂芳基，环烷基或杂环烷基，或-CO 2（烷基或取代的氨基 ）或CN; Z2是H或Z1; Z 3是H或烷基; 或Z 1，Z 2和Z 3与它们所连接的碳一起形成双环饱和或不饱和环;因此，药物组合物以及所述化合物用作疼痛，焦虑，咳嗽，哮喘的伤害感受肽受体抑制剂的用途 ，公开抑郁症和酗酒。

    High affinity ligands for nociceptin receptor ORL-1
    10.
    发明授权
    High affinity ligands for nociceptin receptor ORL-1 有权
    伤害感受器受体ORL-1的高亲和力配体

    公开(公告)号：US06262066B1

    公开(公告)日：2001-07-17

    申请号：US09359771

    申请日：1999-07-26

    申请人： Deen Tulshian ,  Ginny D. Ho ,  Lisa S. Silverman ,  Julius J. Matasi ,  Robbie L. McLeod ,  John A. Hey ,  Richard W. Chapman ,  Ana Bercovici ,  Francis M. Cuss

    发明人： Deen Tulshian ,  Ginny D. Ho ,  Lisa S. Silverman ,  Julius J. Matasi ,  Robbie L. McLeod ,  John A. Hey ,  Richard W. Chapman ,  Ana Bercovici ,  Francis M. Cuss

    IPC分类号： C07D22122

    CPC分类号： A61K45/06 ,  A61K31/00 ,  A61K31/438 ,  A61K31/439 ,  A61K31/451 ,  A61K31/4535 ,  A61K31/454

    摘要： Novel compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: the dotted line represents an optional double bond; X1 is optionally substituted alkyl, cycloalkyl, aryl, heteroaryl or heterocycloalkyl; X2 is —CHO, —CN, optionally substituted amino, alkyl, or aryl; or X1 is optionally substituted benzofused heterocyclyl and X2 is hydrogen; or X1 and X2 together form an optionally benzofused Spiro heterocyclyl group R1, R2, R3 and R4 are independently H and alkyl, or (R1 and R4) or (R2 and R3) or (R1 and R3) or (R2 and R4) together can form an alkylene bridge of 1 to 3 carbon atoms; Z1 is optionally substituted alkyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl, or —CO2(alkyl or substituted amino) or CN; Z2 is H or Z1; Z3 is H oralkyl; or Z1, Z2 and Z3, together with the carbon to which they are attached, form bicyclic saturated or unsaturated rings; pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.

    摘要翻译： 式的新型化合物或其药学上可接受的盐或溶剂化物，其中：虚线表示任选的双键; X 1为任选取代的烷基，环烷基，芳基，杂芳基或杂环烷基; X 2为-CHO，-CN，任选取代的氨基， 烷基或芳基;或X 1为任选取代的苯并稠合的杂环基，且X 2为氢;或X 1和X 2一起形成任选的苯并稠合的螺杂环基R1，R2，R3和R4独立地为H和烷基，或（R1和R4）或 和（R 3和R 3）或（R 1和R 3）或（R 2和R 4）在一起可以形成1至3个碳原子的亚烷基桥; Z 1是任选取代的烷基，芳基，杂芳基，环烷基或杂环烷基，或-CO 2（烷基或取代的氨基 ）或CN; Z2是H或Z1; Z 3是H或烷基; 或Z 1，Z 2和Z 3与它们所连接的碳一起形成双环饱和或不饱和环; 因此，公开了用于治疗疼痛，焦虑，咳嗽，哮喘，抑郁和酒精滥用的所述化合物作为伤害感受肽受体抑制剂的用途。