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1. 发明授权

US06903123B2 Azetidinyl diamines useful as ligands of the nociceptin receptor ORL-1 失效
标题翻译：可用作伤害感受肽受体ORL-1的配体的氮杂环丁烷二胺
公开(公告)号：US06903123B2
公开(公告)日：2005-06-07
申请号：US10770758
申请日：2004-02-03
申请人： Duane A. Burnett , Mary Ann Caplen , Michael F. Czarniecki , Martin S. Domalksi , Ginny D. Ho , Deen Tulshian , Wen-Lian Wu
发明人： Duane A. Burnett , Mary Ann Caplen , Michael F. Czarniecki , Martin S. Domalksi , Ginny D. Ho , Deen Tulshian , Wen-Lian Wu
IPC分类号： A61K31/397 , A61K31/4025 , A61K31/4178 , A61K31/4427 , A61K31/4523 , A61K31/4545 , A61K31/496 , A61K31/506 , A61K45/06 , A61P11/06 , A61P11/14 , A61P25/04 , A61P25/22 , A61P25/24 , A61P25/32 , C07D205/04 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D405/14 , C07D417/06 , C07D521/00 , C07D401/00 , A61K31/40
CPC分类号： C07D231/12 , C07D205/04 , C07D233/56 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D417/06
摘要： Disclosed are nociceptin ORL-1 receptor agonists of the formula wherein: (a) R1 is optionally substituted alkyl, fluorenyl, pyrimidinyl or optionally substituted piperidinyl; R2 is H; and R3 is —C(H)(R)—NR7R8; R is H, optionally substituted aryl or arylalkyl, or heteroaryl; R7 is —(CH2)xR9, optionally substituted tetrahydronaphthyl, or cycloalkyl; and R8 is H; or R7 and R8 together form a substituted piperidinyl or piperazinyl ring; x is 0-10; and R9 is H, alkoxy, optionally substituted phenyl, naphthyl, heteroaryl, pyrrolidinyl, pyrrolidonyl, optionally substituted piperidinyl or diphenylmethyl; or (b) R2 is —NHR7 or and R3 is H; pharmaceutical compositions; and methods of using the compounds to treat cough and pain.
摘要翻译：公开了下式的伤害感受肽ORL-1受体激动剂其中：（a）R 1是任选取代的烷基，芴基，嘧啶基或任选取代的哌啶基; R 2是H; 和R 3是-C（H）（R）-NR 7 R 8; R是H，任选取代的芳基或芳烷基或杂芳基; R 7是 - （CH 2 CH 2）x R 9，任选取代的四氢萘基或环烷基; R 8是H; 或R 7和R 8一起形成取代的哌啶基或哌嗪基环; x为0-10; R 9是H，烷氧基，任选取代的苯基，萘基，杂芳基，吡咯烷基，吡咯烷酮基，任选取代的哌啶基或二苯基甲基; 或（b）R 2是-NHR 7或R 3和R 3是H; 药物组合物; 以及使用该化合物治疗咳嗽和疼痛的方法。

2. 发明申请

US20120028975A1 SUBSTITUTED TRIAZOLOPYRIDINES AND ANALOGS THEREOF 失效
标题翻译：取代三唑并吡啶类及其类似物
公开(公告)号：US20120028975A1
公开(公告)日：2012-02-02
申请号：US13262990
申请日：2010-04-05
申请人： Ginny D. Ho , Elizabeth M. Smith , Eugenia Y. Kiselgof , Kallol Basu , Zheng Tan , Brian McKittrick , Deen Tulshian
发明人： Ginny D. Ho , Elizabeth M. Smith , Eugenia Y. Kiselgof , Kallol Basu , Zheng Tan , Brian McKittrick , Deen Tulshian
IPC分类号： A61K31/437 , A61K31/5377 , A61P25/18 , A61P3/00 , A61P25/28 , A61P25/24 , A61P3/04 , A61P3/10 , C07D471/04 , A61P25/00
CPC分类号： C07D471/04
摘要： The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds.
摘要翻译：本发明涉及取代的三唑并吡啶类及其类似物，该化合物作为磷酸二酯酶10（PDE10）抑制剂用于治疗PDE10调节的病症的药物组合物用于包含该化合物的药物组合物。

3. 发明授权

US06727254B2 Heteroaryl tropane derivatives as superior ligands for nociceptin receptor ORL-1 失效
标题翻译：杂芳基托烷衍生物作为伤害感受肽受体ORL-1的优良配体
公开(公告)号：US06727254B2
公开(公告)日：2004-04-27
申请号：US10288976
申请日：2002-11-06
申请人： Deen Tulshian , Ginny D. Ho , Fay W. Ng
发明人： Deen Tulshian , Ginny D. Ho , Fay W. Ng
IPC分类号： C07D40104
CPC分类号： C07D451/06
摘要： Novel compounds of the formula wherein R is optionally substituted heteroaryl or R1 is H or C1-C6 alkyl; and R2 and R3 are —CH3, —OCH3 or halo; or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions therefore, and the use of said compounds in the treatment of pain, anxiety, cough, asthma, depression and alcohol abuse are disclosed.
摘要翻译：式（Ⅳ）的新化合物是任选取代的杂芳基或R 1是H或C 1 -C 6烷基; 和R 2和R 3是-CH 3，-OCH 3或卤素;或其药学上可接受的盐或溶剂合物，因此药物组合物，以及所述化合物在治疗疼痛，焦虑，咳嗽，哮喘，抑郁症中的用途并公开酗酒。

4. 发明授权

US06716846B2 High affinity ligands for nociceptin receptor ORL-1 失效
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：US06716846B2
公开(公告)日：2004-04-06
申请号：US10155277
申请日：2002-05-23
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： C07D40306
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合物，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，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 3和R 4独立地为H和烷基，或（R 1和R 4）或（R 2和R 3）或（R 1） >和R 3）或（R 2和R 4）可以一起形成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。

5. 发明授权

US07910603B2 3-monosubstituted tropane derivatives as nociceptin receptor ligands 有权
标题翻译： 3-单取代的托烷衍生物作为伤害感受肽受体配体
公开(公告)号：US07910603B2
公开(公告)日：2011-03-22
申请号：US12338384
申请日：2008-12-18
申请人： Ginny D. Ho , Deen Tulshian , Shu-Wei Yang
发明人： Ginny D. Ho , Deen Tulshian , Shu-Wei Yang
IPC分类号： A01N43/42 , A61K31/44
CPC分类号： C07D451/02 , C07D451/04 , C07D451/06
摘要： Compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R1 is aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R2 is H; or aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R3 is aryl, heteroaryl, cycloalkyl or heterocycloalkyl, all optionally substituted; X is a bond, —(CH2)m—N(R7)—(CH2)n—, —(CH2)m—O—(CH2)n—, —(CH2)m—S—(CH2)n—, —C(O)—, —CH(OH)—, —C(O)N(R7)—, —C(O)N(R7)-alkylene or —N(R7)C(O)—; R7 is H or alkyl; and m and n are each 0-6, provided that the sum of m and n is 0-6; or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions thereof, and the use of said compounds in the treatment of cough, pain, anxiety, asthma, depression, alcohol abuse, urinary incontinence and overactive bladder are disclosed.
摘要翻译：其中R1是芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基，环烷基烷基，杂环烷基，杂环烷基烷基或烷基的化合物或其药学上可接受的盐， R2为H; 或芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基，环烷基烷基，杂环烷基，杂环烷基烷基或烷基，全部被取代; R3是芳基，杂芳基，环烷基或杂环烷基，全部被取代; X是一个键， - （CH 2）m -N（R 7） - （CH 2）n - ， - （CH 2）m -O-（CH 2）n - ， - （CH 2）m -S-（CH 2） -C（O） - ， - CH（OH） - ， - C（O）N（R 7） - ， - C（O）N（R 7） - 亚烷基或-N（R 7）C（O） R7是H或烷基; m和n各自为0-6，条件是m和n的和为0-6; 或其药学上可接受的盐或溶剂合物，其药物组合物，以及所述化合物在治疗咳嗽，疼痛，焦虑，哮喘，抑郁，酒精滥用，尿失禁和膀胱过度活动症中的用途。

6. 发明授权

US07485650B2 High affinity ligands for nociceptin receptor ORL-1 失效
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：US07485650B2
公开(公告)日：2009-02-03
申请号：US11259765
申请日：2005-10-27
申请人： David G. Sawutz , Philippe Brianceau , Ana Bercovici , Ginny D. Ho , Deen Tulshian
发明人： David G. Sawutz , Philippe Brianceau , Ana Bercovici , Ginny D. Ho , Deen Tulshian
IPC分类号： A61K31/46
CPC分类号： C07D451/02
摘要： The compound of the formula or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions therefore, and the use of said compounds as nociceptin receptor inhibitors useful in the treatment of anxiety are disclosed.
摘要翻译：公开了式的化合物或其药学上可接受的盐或溶剂化物，因此药物组合物以及所述化合物作为治疗焦虑症的伤害感受肽受体抑制剂的用途。

7. 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。

8. 发明授权

US08685967B2 Substituted triazolopyridines and analogs thereof 失效
标题翻译：取代的三唑并吡啶类及其类似物
公开(公告)号：US08685967B2
公开(公告)日：2014-04-01
申请号：US13262990
申请日：2010-04-05
申请人： Ginny D. Ho , Elizabeth M. Smith , Eugenia Y. Kiselgof , Kallol Basu , Zheng Tan , Brian McKittrick , Deen Tulshian
发明人： Ginny D. Ho , Elizabeth M. Smith , Eugenia Y. Kiselgof , Kallol Basu , Zheng Tan , Brian McKittrick , Deen Tulshian
IPC分类号： A61K31/437 , A61K31/5377 , A61P25/18 , A61P3/00 , A61P25/28 , A61P25/24 , A61P3/04 , A61P3/10 , C07D471/04 , A61P25/00
CPC分类号： C07D471/04
摘要： The present invention relates to substituted triazolopyridines and analogs thereof, the use of the compounds as phosphodiesterase 10 (PDE10) inhibitors for the treatment of PDE10-modulated disorders, to pharmaceutical compositions comprising the compounds.
摘要翻译：本发明涉及取代的三唑并吡啶类及其类似物，该化合物作为磷酸二酯酶10（PDE10）抑制剂用于治疗PDE10调节的病症的药物组合物用于包含该化合物的药物组合物。

9. 发明申请

US20090105248A1 3-MONOSUBSTITUTED TROPANE DERIVATIVES AS NOCICEPTIN RECEPTOR LIGANDS 有权
标题翻译：作为NOCICEPTIN受体配体的3单体TROPANE衍生物
公开(公告)号：US20090105248A1
公开(公告)日：2009-04-23
申请号：US12338384
申请日：2008-12-18
申请人： Ginny D. Ho , Deen Tulshian , Shu-Wei Yang
发明人： Ginny D. Ho , Deen Tulshian , Shu-Wei Yang
IPC分类号： A61K31/506 , C07D239/34 , C07D221/22 , A61K31/5377 , A61P11/14 , A61K31/439 , C07D417/08
CPC分类号： C07D451/02 , C07D451/04 , C07D451/06
摘要： Compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R1 is aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R2 is H; or aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R3 is aryl, heteroaryl, cycloalkyl or heterocycloalkyl, all optionally substituted; X is a bond, —(CH2)m—N(R7)—(CH2)n—, —(CH2)m—O—(CH2)n—, —(CH2)m—S—(CH2)n—, —C(O)—, —CH(OH)—, —C(O)N(R7)—, —C(O)N(R7)-alkylene or —N(R7)C(O)—; R7 is H or alkyl; and m and n are each 0-6, provided that the sum of m and n is 0-6; or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions thereof, and the use of said compounds in the treatment of cough, pain, anxiety, asthma, depression, alcohol abuse, urinary incontinence and overactive bladder are disclosed.
摘要翻译：其中R1是芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基，环烷基烷基，杂环烷基，杂环烷基烷基或烷基的化合物或其药学上可接受的盐， R2为H; 或芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基，环烷基烷基，杂环烷基，杂环烷基烷基或烷基，全部被取代; R3是芳基，杂芳基，环烷基或杂环烷基，全部被取代; X是键， - （CH 2）m N（R 7） - （CH 2）n - ， - （CH 2）m O-（CH 2）n - ， - （CH 2）m -S-（CH 2），-CH（OH） - ， - C（O）N（R7） - ， - C（O）N（R7） - 亚烷基或-N（R7）C（O） - ; R7是H或烷基; m和n各自为0-6，条件是m和n的和为0-6; 或其药学上可接受的盐或溶剂化物，其药物组合物，以及所述化合物在治疗咳嗽，疼痛，焦虑，哮喘，抑郁，酒精滥用，尿失禁和膀胱过度活动症中的用途。

10. 发明授权

US07479494B2 3-monosubstituted tropane derivatives as nociceptin receptor ligands 有权
标题翻译： 3-单取代的托烷衍生物作为伤害感受肽受体配体
公开(公告)号：US07479494B2
公开(公告)日：2009-01-20
申请号：US11589388
申请日：2006-10-30
申请人： Ginny D. Ho , Deen Tulshian , Shu-Wei Yang
发明人： Ginny D. Ho , Deen Tulshian , Shu-Wei Yang
IPC分类号： A01N43/54 , A01N43/42 , C07D239/42 , C07D401/04 , C07D451/00 , C07D401/00 , C07D405/00 , C07D409/00 , C07D239/00 , C07D239/02 , A61K31/44
CPC分类号： C07D451/02 , C07D451/04 , C07D451/06
摘要： Compounds of the formula or a pharmaceutically acceptable salt thereof, wherein R1 is aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R2 is H; or aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, heterocycloalkylalkyl or alkyl, all optionally substituted; R3 is aryl, heteroaryl, cycloalkyl or heterocycloalkyl, all optionally substituted; X is a bond, —(CH2)m—N(R7)—(CH2)n—, —(CH2)m—O—(CH2)n—, —(CH2)m—S—CH2)n—, —C(O)—, —CH(OH)—, —C(O)N(R7)—, —C(O)N(R7)-alkylene or —N(R7)C(O)—; R7 is H or alkyl; and m and n are each 0-6, provided that the sum of m and n is 0-6; or a pharmaceutically acceptable salt or solvate thereof, pharmaceutical compositions thereof, and the use of said compounds in the treatment of cough, pain, anxiety, asthma, depression, alcohol abuse, urinary incontinence and overactive bladder are disclosed.
摘要翻译：其中R1是芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基，环烷基烷基，杂环烷基，杂环烷基烷基或烷基的化合物或其药学上可接受的盐， R2为H; 或芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基，环烷基烷基，杂环烷基，杂环烷基烷基或烷基，全部被取代; R3是芳基，杂芳基，环烷基或杂环烷基，全部被取代; X是键， - （CH 2）m N（R 7） - （CH 2）n - ， - （CH 2）m O-（CH 2）n - ， - （CH 2）m S-CH 2）n - ， - C（O） -CH（OH） - ， - C（O）N（R 7） - ， - C（O）N（R 7） - 亚烷基或-N（R 7）C（O） R7是H或烷基; m和n各自为0-6，条件是m和n的和为0-6; 或其药学上可接受的盐或溶剂化物，其药物组合物，以及所述化合物在治疗咳嗽，疼痛，焦虑，哮喘，抑郁，酒精滥用，尿失禁和膀胱过度活动症中的用途。

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