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1. 发明申请

WO2012145581A1 DISUBSTITUTED OCTAHY-DROPYRROLO [3,4-C] PYRROLES AS OREXIN RECEPTOR MODULATORS 审中-公开
标题翻译：作为OREXIN受体调节剂的衍生化的吡咯并[3,4-C]吡咯
公开(公告)号：WO2012145581A1
公开(公告)日：2012-10-26
申请号：PCT/US2012/034372
申请日：2012-04-20
申请人： JANSSEN PHARMACEUTICA NV , LETAVIC, Michael , RUDOLPH, Dale, A. , SAVALL, Brad, M. , SHIREMAN, Brock, T. , SWANSON, Devin
发明人： LETAVIC, Michael , RUDOLPH, Dale, A. , SAVALL, Brad, M. , SHIREMAN, Brock, T. , SWANSON, Devin
IPC分类号： C07D487/04 , A61K31/407 , A61P25/00
CPC分类号： C07D487/04 , A61K31/421 , A61K31/498 , A61K31/506 , C07D403/04 , C07D403/14 , C07D413/10
摘要： Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
摘要翻译：描述了二取代八氢吡咯并[3,4-c]吡咯化合物，其可用作食欲素受体调节剂。这样的化合物可用于治疗由食欲素活性（例如失眠）介导的疾病状态，病症和病症的药物组合物和方法。

2. 发明申请

WO2006105304A8 PHENYL AND PYRIDYL LTA4H MODULATORS 审中-公开
标题翻译： PHYYY和PYRIDYL LTA4H调节器
公开(公告)号：WO2006105304A8
公开(公告)日：2008-02-07
申请号：PCT/US2006011663
申请日：2006-03-30
申请人： JANSSEN PHARMACEUTICA NV , BUTLER CHRISTOPHER R , EDWARDS JAMES P , FOURIE ANNE M , GRICE CHERYL A , KARLSSON LARS , SAVALL BRAD M , TAYS KEVIN L , WEI JIANMEI
发明人： BUTLER CHRISTOPHER R , EDWARDS JAMES P , FOURIE ANNE M , GRICE CHERYL A , KARLSSON LARS , SAVALL BRAD M , TAYS KEVIN L , WEI JIANMEI
IPC分类号： A61K31/445 , A61K31/135 , A61P29/00 , C07D207/06 , C07D211/44 , C07D211/58 , C07D223/04 , C07D241/08 , C07D265/30 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/12 , C07D471/10
CPC分类号： C07D295/088 , A61K31/135 , A61K31/445 , A61K31/454 , A61K31/4545 , C07C217/60 , C07C229/14 , C07C255/24 , C07C271/58 , C07C2601/02 , C07D207/06 , C07D209/42 , C07D211/12 , C07D211/14 , C07D211/22 , C07D211/40 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/52 , C07D211/58 , C07D211/60 , C07D211/62 , C07D211/76 , C07D213/64 , C07D223/04 , C07D241/08 , C07D265/30 , C07D295/096 , C07D333/36 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D471/10
摘要： Leukotrfene A4 hydrolase (LTA4H) inhibitors, compositions containing them, and methods of use for the inhibition of LTA4H enzyme activity and the treatment, prevention or inhibition of inflammation and inflammatory conditions.
摘要翻译：白细胞素A4水解酶（LTA4H）抑制剂，含有它们的组合物，以及用于抑制LTA4H酶活性和治疗，预防或抑制炎症和炎性病症的方法。

3. 发明申请

WO2014152537A1 P2X7 MODULATORS 审中-公开
标题翻译： P2X7调制器
公开(公告)号：WO2014152537A1
公开(公告)日：2014-09-25
申请号：PCT/US2014/027450
申请日：2014-03-14
申请人： JANSSEN PHARMACEUTICA NV , AMERICKS, Michael K. , RECH, Jason C. , SAVALL, Brad M. , WALL, Jessica L.
发明人： AMERICKS, Michael K. , RECH, Jason C. , SAVALL, Brad M. , WALL, Jessica L.
IPC分类号： C07D487/04 , C07D487/14 , A61K31/4985 , A61P25/00 , A61P19/00 , A61P11/00
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/501 , A61K31/506 , C07D487/14 , Y02A50/414
摘要： The present invention is directed to a compound of Formula (I) Formula (I) The invention also relates to pharmaceutical compositions comprising compounds of Formula (I) and methods comprising administering to a subject at least one compound selected from compounds of Formula (I) for treating diseases mediated by P2X7 receptor activity, such as rheumatoid arthritis, osteoarthritis, psoriasis, septic shock, allergic dermatitis, asthma, allergic asthma, mild to severe asthma, steroid resistant asthma, idiopathic pulmonary fibrosis, allergic rhinitis, chronic obstructive pulmonary disease; airway hyper-responsiveness, diseases of the nervous and neuro-immune system, acute and chronic pain states of neuropathic pain, inflammatory pain, spontaneous pain, opioid induced pain, diabetic neuropathy, postherpetic neuralgia, low back pain, chemotherapy-induced neuropathic pain, fibromyalgia, diseases involved with and without neuroinflammation of the central nervous system, mood disorders, major depression, major depressive disorder, treatment resistant depression, bipolar disorder, anxious depression, anxiety, cognition, sleep disorders, multiple sclerosis, epileptic seizures, Parkinson's disease, schizophrenia, Alzheimer's disease, Huntington's disease, autism, spinal cord injury and cerebral ischemia/traumatic brain injury, stress-related disorders, diseases of the cardiovascular, metabolic, gastrointestinal and urogenital systems such as diabetes, diabetes mellitus, thrombosis, irritable bowel syndrome, irritable bowel disease, Crohn's disease, ischemic heart disease, ischaemia, hypertension, cardiovascular disease, myocardial infarction, and lower urinary tract dysfunction such as incontinence, lower urinary tract syndrome, Polycystic Kidney Disease, Glomerulonephritis, skeletal disorders, osteoporosis, osteopetrosis, and glaucoma, interstitial cystitis, cough, ureteric obstruction, sepsis, Amyotrophic Lateral Sclerosis, Chaga's Disease, chlamydia, neuroblastoma, Tuberculosis, and migraine.
摘要翻译：本发明涉及式（I）化合物（I）本发明还涉及包含式（I）化合物的药物组合物和方法，其包括向受试者施用至少一种选自式（I）化合物的化合物，用于治疗由P2X7受体活性介导的疾病，例如类风湿性关节炎，骨关节炎，牛皮癣，败血性休克，过敏性皮炎，哮喘，过敏性哮喘，轻度至重度哮喘，类固醇抗性哮喘，特发性肺纤维化，过敏性鼻炎，慢性阻塞性肺病; 气道高反应性，神经和神经免疫系统疾病，神经性疼痛的急性和慢性疼痛状态，炎性疼痛，自发性疼痛，阿片样物质诱导的疼痛，糖尿病性神经病，带状疱疹后神经痛，腰痛，化疗诱发的神经性疼痛，纤维肌痛，涉及和不伴有中枢神经系统神经炎症的疾病，情绪障碍，重度抑郁症，重度抑郁障碍，耐药抑郁症，双相情感障碍，焦虑抑郁症，焦虑症，认知障碍，睡眠障碍，多发性硬化，癫痫发作，帕金森病，精神分裂症，阿尔茨海默氏病，亨廷顿病，自闭症，脊髓损伤和脑缺血/创伤性脑损伤，应激相关疾病，心血管疾病，代谢，胃肠道和泌尿生殖系统如糖尿病，糖尿病，血栓形成，肠易激综合征，肠易激综合征，克罗恩病，缺血性心脏病，脊髓多发性肾脏疾病，肾小球性肾炎，骨骼疾病，骨质疏松症，骨质疏松症，青光眼，间质性膀胱炎，咳嗽，输尿管梗阻，败血症，脓毒症，肌萎缩性侧索硬化症，卡加氏病，衣原体，神经母细胞瘤，结核病和偏头痛。

4. 发明申请

WO2011050202A1 FUSED HETEROCYCLIC COMPOUNDS AS OREXIN RECEPTOR MODULATORS 审中-公开
标题翻译：熔化的杂环化合物作为OREXIN受体调节剂
公开(公告)号：WO2011050202A1
公开(公告)日：2011-04-28
申请号：PCT/US2010/053611
申请日：2010-10-21
申请人： JANSSEN PHARMACEUTICA NV , BRANSTETTER, Bryan, James , LETAVIC, Michael, A. , LY, Kiev, S. , RUDOLPH, Dale, A. , SAVALL, Brad, M. , SHAH, Chandravadan, R. , SHIREMAN, Brock, T.
发明人： BRANSTETTER, Bryan, James , LETAVIC, Michael, A. , LY, Kiev, S. , RUDOLPH, Dale, A. , SAVALL, Brad, M. , SHAH, Chandravadan, R. , SHIREMAN, Brock, T.
IPC分类号： C07D471/04 , C07D487/04 , A61K31/4353 , A61P25/00
CPC分类号： C07D471/04 , C07D487/04
摘要： Certain disubstituted 3,8-diaza-bicyclo[4.2.0]octane and 3,6-diazabicyclo [3.2.0]heptane are described, which are useful as orexin inhibitors. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
摘要翻译：描述了某些二取代的3,8-二氮杂 - 双环[4.2.0]辛烷和3,6-二氮杂双环[3.2.0]庚烷，其可用作食欲素抑制剂。这样的化合物可用于治疗由食欲素活性（例如失眠）介导的疾病状态，病症和病症的药物组合物和方法。

5. 发明申请

WO2011050200A1 FUSED HETEROCYCLIC COMPOUNDS AS OREXIN RECEPTOR MODULATORS 审中-公开
标题翻译：熔化的杂环化合物作为OREXIN受体调节剂
公开(公告)号：WO2011050200A1
公开(公告)日：2011-04-28
申请号：PCT/US2010/053609
申请日：2010-10-21
申请人： JANSSEN PHARMACEUTICA NV , BRANSTETTER, Bryan, James , LETAVIC, Michael, A. , LY, Kiev, S. , RUDOLPH, Dale, A. , SAVALL, Brad, M. , SHAH, Chandravadan, R. , SHIREMAN, Brock, T.
发明人： BRANSTETTER, Bryan, James , LETAVIC, Michael, A. , LY, Kiev, S. , RUDOLPH, Dale, A. , SAVALL, Brad, M. , SHAH, Chandravadan, R. , SHIREMAN, Brock, T.
IPC分类号： C07D471/08 , A61K31/439 , A61P25/00
CPC分类号： C07D471/08
摘要： Disubstituted 3,8-diaza-bicyclo[4.2.0]octane and 3,6-diazabicyclo [3.2.0]heptane compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.
摘要翻译：描述了二取代的3,8-二氮杂双环[4.2.0]辛烷和3,6-二氮杂双环[3.2.0]庚烷化合物，其可用作食欲素受体调节剂。这样的化合物可用于治疗由食欲素活性（例如失眠）介导的疾病状态，病症和病症的药物组合物和方法。

6. 发明申请

WO2008100565A1 2-AMINOPYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR 审中-公开
标题翻译：组胺H4受体的2-氨基嘧啶调节剂
公开(公告)号：WO2008100565A1
公开(公告)日：2008-08-21
申请号：PCT/US2008/001950
申请日：2008-02-14
申请人： JANSSEN PHARMACEUTICA N.V. , CAI, Hui , CHAVEZ, Frank , EDWARDS, James, P. , FITZGERALD, Anne, E. , LIU, Jing , MANI, Neelakandha, S. , NEFF, Danielle, K. , RIZZOLIO, Michele, C. , SAVALL, Brad, M. , SMITH, Deborah, M. , VENABLE, Jennifer, D. , WEI, Jianmei , WOLIN, Ronald, L.
发明人： CAI, Hui , CHAVEZ, Frank , EDWARDS, James, P. , FITZGERALD, Anne, E. , LIU, Jing , MANI, Neelakandha, S. , NEFF, Danielle, K. , RIZZOLIO, Michele, C. , SAVALL, Brad, M. , SMITH, Deborah, M. , VENABLE, Jennifer, D. , WEI, Jianmei , WOLIN, Ronald, L.
IPC分类号： A01N43/40 , A61K31/445
CPC分类号： C07D498/04 , C07D239/48 , C07D239/70 , C07D239/95 , C07D401/04 , C07D403/04 , C07D405/04 , C07D405/14 , C07D409/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D487/10 , C07D519/00
摘要： 2-Aminopyrimidine compounds are described, which are useful as H 4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H 4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
摘要翻译：描述了2-氨基嘧啶化合物，其可用作H 4 S受体调节剂。这样的化合物可以用于治疗由H 4 S受体活性介导的疾病状态，病症和病症的药物组合物和方法，例如过敏，哮喘，自身免疫疾病和瘙痒症。

7. 发明申请

WO2014152604A1 P2X7 MODULATORS 审中-公开
标题翻译： P2X7调制器
公开(公告)号：WO2014152604A1
公开(公告)日：2014-09-25
申请号：PCT/US2014/027522
申请日：2014-03-14
申请人： JANSSEN PHARMACEUTICA NV , ALCAZAR VACA, Manuel Jesus , ALLISON, Brett, D. , ANDRES GIL, Jose Ignacio , CHROVIAN, Christa, C. , COATE, Heather, R. , DE ANGELIS, Meri , DENG, Xiaohu , DVORAK, Curt, A. , GELIN, Christine, F. , LETAVIC, Michael, A. , LIANG, Jimmy, T. , MANI, Neelakandha, S. , RECH, Jason, C. , SAVALL, Brad, M. , SOYODE-JOHNSON, Akinola , STENNE, Brice, M. , SWANSON, Devin, M. , WALL, Jessica, L.
发明人： ALCAZAR VACA, Manuel Jesus , ALLISON, Brett, D. , ANDRES GIL, Jose Ignacio , CHROVIAN, Christa, C. , COATE, Heather, R. , DE ANGELIS, Meri , DENG, Xiaohu , DVORAK, Curt, A. , GELIN, Christine, F. , LETAVIC, Michael, A. , LIANG, Jimmy, T. , MANI, Neelakandha, S. , RECH, Jason, C. , SAVALL, Brad, M. , SOYODE-JOHNSON, Akinola , STENNE, Brice, M. , SWANSON, Devin, M. , WALL, Jessica, L.
IPC分类号： C07D471/04 , A61K31/437 , A61P29/00 , A61P37/02
CPC分类号： C07D471/04 , A61K31/497 , C07B2200/07 , C07D401/14 , C07F7/0812 , Y02A50/414
摘要： The present invention is directed to compounds of Formulas (I, la, lla and IIb). The invention also relates to pharmaceutical compositions comprising compounds of Formulas (I, la, lla and IIb). Methods of making and using the compounds of Formulas (I, la, lla and IIb) are also within the scope of the invention.
摘要翻译：本发明涉及式（I，Ia，11a和IIb）的化合物。本发明还涉及包含式（I，Ia，11a和IIb）化合物的药物组合物。制备和使用式（I，Ia，11a和IIb）化合物的方法也在本发明的范围内。

8. 发明申请

WO2008008359A2 BENZOFURO-AND BENZOTHIENOPYRYIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR 审中-公开
标题翻译：组胺H4受体的苯并呋喃和苯并噻吩并嘧啶调节剂
公开(公告)号：WO2008008359A2
公开(公告)日：2008-01-17
申请号：PCT/US2007015763
申请日：2007-07-10
申请人： JANSSEN PHARMACEUTICA NV , CHAVEZ FRANK , CURTIS MICHAEL P , EDWARDS JAMES P , GOMEZ LAURENT , GRICE CHERYL A , KEARNEY AARON M , SAVALL BRAD M , FITZGERALD ANNE E , LIU JING , MANI NEELAKANDHA S
发明人： CHAVEZ FRANK , CURTIS MICHAEL P , EDWARDS JAMES P , GOMEZ LAURENT , GRICE CHERYL A , KEARNEY AARON M , SAVALL BRAD M , FITZGERALD ANNE E , LIU JING , MANI NEELAKANDHA S
IPC分类号： A61K31/4985 , A61K31/519 , A61P1/00 , A61P5/00 , A61P9/00 , A61P17/00 , A61P27/00 , A61P37/00 , C07D239/70 , C07D403/14
CPC分类号： C07D491/048 , C07D491/147 , C07D495/04 , C07D519/00
摘要： Benzofuro- and benzothienopyrimidine compounds are described, which are useful as H4 receptor modulators. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.
摘要翻译：描述了苯并呋喃和苯并噻吩并嘧啶化合物，其可用作H 4受体调节剂。这些化合物可用于治疗由H 4受体活性介导的疾病状态，病症和病症的药物组合物和方法，例如过敏，哮喘，自身免疫性疾病和瘙痒症。

9. 发明申请

WO2005012297A9 BENZIMIDAZOLE, BENZTHIAZOLE AND BENZOXAZOLE DERIVATIVES AND THEIR USE AS LTA4H MODULATORS 审中-公开
标题翻译：苯并咪唑，苯并唑和苯并噻唑衍生物及其作为LTA4H调节剂的用途
公开(公告)号：WO2005012297A9
公开(公告)日：2007-01-04
申请号：PCT/US2004024309
申请日：2004-07-27
申请人： JANSSEN PHARMACEUTICA NV , AXE FRANK U , BEMBENEK SCOTT D , BUTLER CHRISTOPHER R , EDWARDS JAMES P , FOURIE ANNE M , GRICE CHERYL A , SAVALL BRAD M , TAYS KEVIN L , WEI JIANMEI
发明人： AXE FRANK U , BEMBENEK SCOTT D , BUTLER CHRISTOPHER R , EDWARDS JAMES P , FOURIE ANNE M , GRICE CHERYL A , SAVALL BRAD M , TAYS KEVIN L , WEI JIANMEI
IPC分类号： C07D235/26 , A61P29/00 , C07D263/58 , C07D277/68 , C07D401/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D495/10
CPC分类号： C04B35/632 , C07D235/26 , C07D263/58 , C07D277/68 , C07D401/12 , C07D413/12 , C07D417/12 , C07D417/14 , C07D495/10
摘要： Leukotriene A4 hydrolase (LTA4H) inhibitors of Formula (I), compositions containing them, and their use for the inhibition of LTA4H enzyme activity and the treatment, prevention or inhibition of inflammation and/or conditions associated with inflammation. Wherein X is selected from the group consisting of NR 5, O, and S, with R 5 being on of H and CH 3; Y is selected from the group consisting; W is selected from the group consisting Of CH 2 and CHR 1 -CH 2, with R 1 being one H and OH, wherein R 1 -attached carbon member in said CHR 1 -CH 2 is not directly attached; R 4 is selected from the group consisting of H, OCH 3 , CI, F Br, OH, NH 2 , CN, CF 3 and CH 3 ; R 6 is H or F; and R 2 and R 3 are each independently selected from various groups.
摘要翻译：式（I）的白三烯A4水解酶（LTA4H）抑制剂，含有它们的组合物及其用于抑制LTA4H酶活性以及治疗，预防或抑制与炎症有关的炎症和/或病症的用途。其中X选自NR 5，O和S，R 5为H和CH 3; Y选自： W选自CH 2和CHR 1 - CH 2，其中R 1是1。 H和OH，其中所述CHR 1 -CH 2 2中的R 1 - 1个碳成员不直接连接; R 4选自H，OCH 3，Cl，F Br，OH，NH 2，CN，CF _{3 和CH 3 3; R 6是H或F; R 2和R 3各自独立地选自不同的基团。}

10. 发明申请

WO2006105304A2 PHENYL AND PYRIDYL LTA4H MODULATORS 审中-公开
标题翻译： PHYYY和PYRIDYL LTA4H调节器
公开(公告)号：WO2006105304A2
公开(公告)日：2006-10-05
申请号：PCT/US2006011663
申请日：2006-03-30
申请人： JANSSEN PHARMACEUTICA NV , BUTLER CHRISTOPHER R , EDWARDS JAMES P , FOURIE ANNE M , GRICE CHERYL A , KARLSSON LARS , SAVALL BRAD M , TAYS KEVIN L , WEI JIANMEI
发明人： BUTLER CHRISTOPHER R , EDWARDS JAMES P , FOURIE ANNE M , GRICE CHERYL A , KARLSSON LARS , SAVALL BRAD M , TAYS KEVIN L , WEI JIANMEI
IPC分类号： A61K31/445 , A61K31/135 , C07D211/44 , C07D401/04
CPC分类号： C07D295/088 , A61K31/135 , A61K31/445 , A61K31/454 , A61K31/4545 , C07C217/60 , C07C229/14 , C07C255/24 , C07C271/58 , C07C2601/02 , C07D207/06 , C07D209/42 , C07D211/12 , C07D211/14 , C07D211/22 , C07D211/40 , C07D211/42 , C07D211/44 , C07D211/46 , C07D211/52 , C07D211/58 , C07D211/60 , C07D211/62 , C07D211/76 , C07D213/64 , C07D223/04 , C07D241/08 , C07D265/30 , C07D295/096 , C07D333/36 , C07D401/04 , C07D401/12 , C07D401/14 , C07D471/04 , C07D471/10
摘要： Leukotriene A4 hydrolase (LTA4H) inhibitors, compositions containing them, and methods of use for the inhibition of LTA4H enzyme activity and the treatment, prevention or inhibition of inflammation and inflammatory conditions.
摘要翻译：白细胞三烯A4水解酶（LTA4H）抑制剂，含有它们的组合物，以及用于抑制LTA4H酶活性和治疗，预防或抑制炎症和炎性病症的方法。

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