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1. 发明申请

US20120316176A1 DERIVATIVES OF 7,8-DIHYDRO-1H-IMIDAZO[2,1-b] PURIN-4(5H)-ONE and METHODS OF USE THEREOF 审中-公开
标题翻译： 7,8-二氢-1H-咪唑并[2,1-b]嘌呤-4（5H）酮的衍生物及其使用方法
公开(公告)号：US20120316176A1
公开(公告)日：2012-12-13
申请号：US13517442
申请日：2010-12-16
申请人： Deen Tulshian , Michael F. Czarniecki , Julius Matasi , Stephanie N. Brumfield
发明人： Deen Tulshian , Michael F. Czarniecki , Julius Matasi , Stephanie N. Brumfield
IPC分类号： C07D487/14 , A61P11/00 , A61P19/02 , A61P11/06 , A61K31/519 , A61P29/00
CPC分类号： C07D487/12
摘要： The present invention relates to derivatives of 7,8-dihydro-1H-imidazo[2,1-b]purin-4(5H)-one, compositions thereof and methods of use thereof for treating or preventing pain or an inflammatory disease.
摘要翻译：本发明涉及7,8-二氢-1H-咪唑并[2,1-b]嘌呤-4（5H） - 酮的衍生物及其用于治疗或预防疼痛或炎性疾病的组合物及其用途。

2. 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。

3. 发明授权

US4971972A Phosphodiesterase inhibitors having an optionally substituted purine derivative portion and a benzo- or cyclopenta-furan portion 失效
标题翻译：具有任选取代的嘌呤衍生物部分和苯并或环戊呋喃部分的磷酸二酯酶抑制剂
公开(公告)号：US4971972A
公开(公告)日：1990-11-20
申请号：US327638
申请日：1989-03-23
申请人： Ronald J. Doll , Deen Tulshian , Charles V. Magatti
发明人： Ronald J. Doll , Deen Tulshian , Charles V. Magatti
IPC分类号： C07D473/00
CPC分类号： C07D473/00
摘要： Antihypertensive phosphodiesterase inhibitors having an optionally substituted purine derivative portion and a benzo- or cyclopenta-furan derivative portion are disclosed.
摘要翻译：公开了具有任选取代的嘌呤衍生物部分和苯并或环戊呋喃衍生物部分的抗高血压磷酸二酯酶抑制剂。

4. 发明申请

US20140194404A1 AMIDOPYRAZOLE INHIBITORS OF INTERLEUKIN RECEPTOR-ASSOCIATED KINASES 有权
标题翻译：白介素受体相关激酶的氨基吡唑抑制剂
公开(公告)号：US20140194404A1
公开(公告)日：2014-07-10
申请号：US14006565
申请日：2012-03-21
申请人： William T. McElroy , Guoqing Li , Ginny Dai Ho , Zheng Tan , Sunil Paliwal , William Michael Seganish , Deen Tulshian , John Lampe , Joey L. Methot , Hua Zhou , Michael D. Altman , Liang Zhu
发明人： William T. McElroy , Guoqing Li , Ginny Dai Ho , Zheng Tan , Sunil Paliwal , William Michael Seganish , Deen Tulshian , John Lampe , Joey L. Methot , Hua Zhou , Michael D. Altman , Liang Zhu
IPC分类号： C07D487/04
CPC分类号： C07D487/04 , A61K31/4162
摘要： This invention relates to amidopyrazole compounds that are inhibitors of Interleukin receptor-associated kinases, in particular IRAK-4, and are useful in the treatment of cellular proliferative diseases, for example, cancer, hyperplasia, restenosis, cardiac hypertrophy, immune disorders and inflammation.
摘要翻译：本发明涉及作为白介素受体相关激酶抑制剂，特别是IRAK-4的氨基吡唑化合物，可用于治疗细胞增殖性疾病，例如癌症，增生，再狭窄，心脏肥大，免疫疾病和炎症。

5. 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。

6. 发明申请

US20080089858A1 AZETIDINE DERIVATIVES USEFUL IN TREATING PAIN, DIABETES AND DISORDERS OF LIPID METABOLISM 失效
标题翻译：适用于治疗脂肪代谢的疼痛，糖尿病和疾病的AZETIDINE衍生物
公开(公告)号：US20080089858A1
公开(公告)日：2008-04-17
申请号：US11854600
申请日：2007-09-13
申请人： Brian McKittrick , Elizabeth Smith , Chad Bennett , Joel Harris , Eugenia Kiselgof , Chad Knutson , Peter Korakas , Deen Tulshian , Hyunjin Kim
发明人： Brian McKittrick , Elizabeth Smith , Chad Bennett , Joel Harris , Eugenia Kiselgof , Chad Knutson , Peter Korakas , Deen Tulshian , Hyunjin Kim
IPC分类号： A61K31/438 , A61K31/565 , A61K31/57 , A61K31/573 , A61K31/675 , A61K38/20 , A61P3/10 , C07D471/10
CPC分类号： C07D471/08
摘要： Disclosed are compounds of the formula: and compounds of the formula: wherein R1, R2, R3, R4, R5, u and v are as defined herein. Also disclosed are methods of treating pain (e.g., inflammatory pain, chronic pain, and neuropathic pain), methods of treating diabetes, and methods of inhibiting the absorption of cholesterol using compounds of formula I or IIA.
摘要翻译：公开了下式的化合物和下式的化合物：其中R 1，R 2，R 3，R 4， u，v和u如本文所定义。还公开了治疗疼痛（例如炎性疼痛，慢性疼痛和神经性疼痛）的方法，治疗糖尿病的方法，以及使用式I或IIA化合物抑制胆固醇吸收的方法。

7. 发明申请

US20060217414A1 High affinity ligands for nociceptin receptor ORL-1 失效
公开(公告)号：US20060217414A1
公开(公告)日：2006-09-28
申请号：US11259765
申请日：2005-10-27
申请人： David Sawutz , Philippe Brianceau , Ana Bercovici , Ginny Ho , Deen Tulshian
发明人： David Sawutz , Philippe Brianceau , Ana Bercovici , Ginny Ho , Deen Tulshian
IPC分类号： C07D453/02 , 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.

8. 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。}

9. 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。

10. 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。

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