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1. 发明授权

US06653315B2 Adenosine A2a receptor antagonists 有权
标题翻译：腺苷A2a受体拮抗剂
公开(公告)号：US06653315B2
公开(公告)日：2003-11-25
申请号：US10269754
申请日：2002-10-11
申请人： Deen Tulshian , Lisa S. Silverman , Julius J. Matasi , Eugenia Y. Kiselgof , John P. Caldwell
发明人： Deen Tulshian , Lisa S. Silverman , Julius J. Matasi , Eugenia Y. Kiselgof , John P. Caldwell
IPC分类号： C07D48714
CPC分类号： C07D487/14 , A61K31/198 , A61K31/505 , A61K45/06 , Y02P20/582 , A61K2300/00
摘要： Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl or heteroaryl, cycloalkenyl, —C(═CH2)CH3, —C≡C—CH3, —CH═C(CH3)2, X is alkylene, —C(O)CH2— or —C(O)N(R2)CH2—; Y is —N(R2)CH2CH2N(R3)—, —OCH2CH2N(R2)—, —O—, —S—, —CH2S—, —(CH2)2—N(R2)—, or optionally substituted divalent heteroaryl, piperidinyl or piperazinyl; and Z is optionally substituted phenyl, phenylalkyl or heteroaryl, diphenylmethyl or R6—C(O)—; or when Y is Z is also R6—SO2—, R7—N(R8)—C(O)—, R7—N(R8)—C(S)— or R6OC(O)—; or when Y is 4-piperidinyl, Z can be phenylamino or pyridylamino; or Z and Y together are substituted piperidinyl, substituted pyrrolidinyl or substituted phenyl; R14 is H, halogen or optionally substituted alkyl; and Q, Q1, m, n, R2, R3, R4, R6, R7 and R8 are as defined in the specification are disclosed, their use in the treatment of Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
摘要翻译：具有结构式I的化合物或其药学上可接受的盐，其中R是任选取代的苯基或杂芳基，环烯基，-C（= CH 2）CH 3，-C = C-CH 3，-CH = C（CH 3）2，X是亚烷基， -C（O）CH 2 - 或-C（O）N（R 2）CH 2 - ; Y是-N（R 2）CH 2 CH 2 N（R 3） - ，-OCH 2 CH 2 N（R 2） - ， - O - ， - S - ， - CH 2 S - ， - （CH 2）2 -N（R 2） - 或任选取代的二价杂芳基，哌啶基或哌嗪基; 和Z是任选取代的苯基，苯基烷基或杂芳基，二苯基甲基或R 6 -C（O） - ;或当Y是Z时也是R 6 -SO 2 - ，R 7 -N（R 8） C（O） - ，R 7 -N（R 8）-C（S） - 或R 6 OC（O） - ;或当Y是4-哌啶基时，Z可以是苯基氨基或吡啶基氨基; 或Z和Y一起是取代的哌啶基，取代的吡咯烷基或取代的苯基; R 14是H，卤素或任选取代的烷基; 和Q，Q 1，m，n，R 2，R 3，R 4，R 6，R 7和R 8如说明书中所定义，它们用于治疗帕金森氏病，单独或与其他治疗帕金森病的药物组合，以及包含它们的药物组合物。

2. 发明授权

US07041666B2 Adenosine A2a receptor antagonists 有权
标题翻译：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。}

3. 发明申请

US20090082336A1 mGluR1 Antagonists as Therapeutic Agents 审中-公开
标题翻译： mGluR1拮抗剂作为治疗剂
公开(公告)号：US20090082336A1
公开(公告)日：2009-03-26
申请号：US12264676
申请日：2008-11-04
申请人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Donalski
发明人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Donalski
IPC分类号： A61K31/55 , C07D495/14 , A61K31/519 , C12N5/06 , A61K31/5377
CPC分类号： C07D471/14 , C07D491/14 , C07D495/04 , C07D495/14 , C09B57/00
摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
摘要翻译：在其许多实施方案中，本发明提供用作代谢型谷氨酸受体（mGluR）拮抗剂的式I（其中J1-J4，X和R1-R5如本文所定义）的三环化合物，特别是作为选择性代谢型谷氨酸受体1拮抗剂，含有该化合物的药物组合物，以及使用该化合物和组合物治疗与代谢型谷氨酸受体（例如，mGluR1）相关的疾病例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默病的治疗方法。

4. 发明授权

US06455527B2 High affinity ligands for nociceptin receptor ORL-1 有权
标题翻译：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。

5. 发明授权

US06262066B1 High affinity ligands for nociceptin receptor ORL-1 有权
标题翻译：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。

6. 发明授权

US07598259B2 mGluR1 antagonists as therapeutic agents 失效
公开(公告)号：US07598259B2
公开(公告)日：2009-10-06
申请号：US11301672
申请日：2005-12-13
申请人： Julius J Matasi , Deen Tulshian , Duane A Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
发明人： Julius J Matasi , Deen Tulshian , Duane A Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D471/00 , C07D487/00 , C07D491/00
CPC分类号： C07D495/14
摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

7. 发明授权

US07485648B2 mGluR1 antagonists as therapeutic agents 失效
标题翻译： mGluR1拮抗剂作为治疗剂
公开(公告)号：US07485648B2
公开(公告)日：2009-02-03
申请号：US11152535
申请日：2005-06-14
申请人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
发明人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
IPC分类号： A01N43/54 , A61K31/505 , C07D471/00 , C07D487/00 , C07D491/00
CPC分类号： C07D471/14 , C07D491/14 , C07D495/04 , C07D495/14 , C09B57/00
摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1—R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
摘要翻译：在其许多实施方案中，本发明提供用作代谢型谷氨酸受体（mGluR）拮抗剂的式I（其中J1-J4，X和R1-R5如本文所定义）的三环化合物，特别是作为选择性代谢型谷氨酸受体1拮抗剂，含有该化合物的药物组合物，以及使用该化合物和组合物治疗与代谢型谷氨酸受体（例如，mGluR1）相关的疾病例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默病的治疗方法。

8. 发明授权

US07094784B2 High affinity ligands for nociceptin receptor ORL-1 有权
标题翻译：伤害感受器受体ORL-1的高亲和力配体
公开(公告)号：US07094784B2
公开(公告)日：2006-08-22
申请号：US10761977
申请日：2004-01-21
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： C07D401/04 , A61K31/46
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：新型式的化合物或其药学上可接受的盐或溶剂合物，其中：虚线表示任选的双键; X 1是任选取代的烷基，环烷基，芳基，杂芳基或杂环烷基; X 2是-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，X 2是氢; 或X 1和X 2一起形成任选的苯并稠合的螺杂环基R 1，R 2，R 2，或者R 4和R 4独立地是H和烷基，或者（R 1和R 4）和（R 0）或者R 2和R 3）或（R 1和R 3）或（R 2）和R 4）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; Z 2是H或Z 1; 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。

9. 发明授权

US07989464B2 mGluR1 antagonists as therapeutic agents 失效
标题翻译： mGluR1拮抗剂作为治疗药
公开(公告)号：US07989464B2
公开(公告)日：2011-08-02
申请号：US12356867
申请日：2009-01-21
申请人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
发明人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
IPC分类号： A01N43/54 , A61K31/505 , C07D239/00 , C07D471/00 , C07D487/00
CPC分类号： C07D495/14
摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
摘要翻译：在其许多实施方案中，本发明提供用作代谢型谷氨酸受体（mGluR）拮抗剂的式I（其中J1-J4，X和R1-R5如本文所定义）的三环化合物，特别是作为选择性代谢型谷氨酸受体1拮抗剂，含有该化合物的药物组合物，以及使用该化合物和组合物治疗与代谢型谷氨酸受体（例如，mGluR1）相关的疾病例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默病的治疗方法。

10. 发明申请

US20090192178A1 mGluR1 ANTAGONISTS AS THERAPEUTIC AGENTS 失效
标题翻译： mGluR1拮抗剂作为治疗药物
公开(公告)号：US20090192178A1
公开(公告)日：2009-07-30
申请号：US12356867
申请日：2009-01-21
申请人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
发明人： Julius J. Matasi , Deen Tulshian , Duane A. Burnett , Wen-Lian Wu , Peter Korakas , Lisa S. Silverman , Thavalakulamgara K. Sasikumar , Li Qiang , Martin S. Domalski
IPC分类号： A61K31/519 , C07D495/14 , A61P25/00
CPC分类号： C07D495/14
摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J4, X, and R1-R5 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.
摘要翻译：在其许多实施方案中，本发明提供用作代谢型谷氨酸受体（mGluR）拮抗剂的式I（其中J1-J4，X和R1-R5如本文所定义）的三环化合物，特别是作为选择性代谢型谷氨酸受体1拮抗剂，含有该化合物的药物组合物，以及使用该化合物和组合物治疗与代谢型谷氨酸受体（例如，mGluR1）相关的疾病例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默病的治疗方法。

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