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1. 发明申请

WO2013012871A1 PROCESSES FOR THE PREPARATION OF PERIPHERAL OPIOID ANTAGONIST COMPOUNDS AND INTERMEDIATES THERETO 审中-公开
标题翻译：制备外周阿片类拮抗剂化合物及其中间体的方法
公开(公告)号：WO2013012871A1
公开(公告)日：2013-01-24
申请号：PCT/US2012/047082
申请日：2012-07-17
申请人： ADOLOR CORPORATION , DOLLE, Roland, E. , LE BOURDONNEC, Bertrand , MARTIN, Pierre , MOESSNER, Christian Steffen , SPINDLER, Felix, Herbert , SPIELVOGEL, Dirk, Jost
发明人： DOLLE, Roland, E. , LE BOURDONNEC, Bertrand , MARTIN, Pierre , MOESSNER, Christian Steffen , SPINDLER, Felix, Herbert , SPIELVOGEL, Dirk, Jost
IPC分类号： A01N43/40
CPC分类号： C07D211/22 , C07D241/44 , C07D317/62
摘要： Novel processes for the preparation of peripheral opioid antagonist compounds and intermediates thereto. The compounds prepared by the present processes may be useful, for example, as antagonists to the mu, kappa and delta opioid receptors, and thereby may be useful in the treatment of gastrointestinal motility disorders, and in preventing peripheral opiate induced side effects. The present processes may offer improved yields, chemical or stereochemical purity, ease of preparation and/or isolation of intermediates and final product, and more industrially useful reaction conditions and workability.
摘要翻译：用于制备外周阿片样物质拮抗剂化合物及其中间体的新方法。通过本发明方法制备的化合物可用作例如mu，κ和δ阿片样物质受体的拮抗剂，因此可用于治疗胃肠动力障碍，以及用于预防外周鸦片诱导的副作用。本方法可以提供改进的产率，化学或立体化学纯度，中间体和最终产物的制备和/或分离的容易程度，以及更具有工业上有用的反应条件和可加工性。

2. 发明申请

WO2011035142A1 USE OF OPIOID RECEPTOR ANTAGONIST FOR GASTROINTESTINAL TRACT DISORDERS 审中-公开
标题翻译：使用阿片受体拮抗剂治疗胃肠疾病
公开(公告)号：WO2011035142A1
公开(公告)日：2011-03-24
申请号：PCT/US2010/049311
申请日：2010-09-17
申请人： ADOLOR CORPORATION , WOODWARD, Richard, M.
发明人： WOODWARD, Richard, M.
IPC分类号： A61K31/497 , A61P1/10
CPC分类号： A61K31/497
摘要： The disclosure relates to a method of treating or preventing a condition in a subject associated with the activation of an opioid receptor in the periphery by administering an effective amount of 5-(2-methoxy-4-{[2-(tetrahydro-pyran-4-yl)-ethylamino]-methyl}-phenoxy)-pyrazine-2-carboxamide (Compound I). In particular, the disclosure relates to a method of treating or preventing opioid- induced constipation or opioid-induced bowel dysfunction in a human without reducing centrally-mediated opioid analgesia or producing central opioid withdrawal symptoms by administering an effective amount of Compound (I). The disclosure further relates to the use of Compound (I) for the preparation of a medicament for the treatment or prevention of a condition in a subject associated with the activation of an opioid receptor in the periphery.
摘要翻译：本公开内容涉及通过施用有效量的5-（2-甲氧基-4 - {[2-（四氢 - 吡喃-2-基） - 哌嗪-1-基）吡啶-4-基） - 乙基氨基] - 甲基} - 苯氧基） - 吡嗪-2-甲酰胺（化合物I）。特别地，本公开涉及一种治疗或预防人类阿片样物质诱发的便秘或阿片样物质诱导的肠功能障碍的方法，而不通过施用有效量的化合物（I）而中和阿片样镇痛或产生中枢阿片样物质戒断症状。本公开还涉及化合物（I）用于制备用于治疗或预防与外周激素相关的阿片样物质受体相关受试者的病症的药物的用途。

3. 发明申请

WO2008033299A2 METHODS FOR ENHANCING COGNITIVE FUNCTION 审中-公开
标题翻译：增强认知功能的方法
公开(公告)号：WO2008033299A2
公开(公告)日：2008-03-20
申请号：PCT/US2007/019661
申请日：2007-09-07
申请人： ADOLOR CORPORATION , DOLLE, Roland, E. , LeBOURDONNEC, Bertrand
发明人： DOLLE, Roland, E. , LeBOURDONNEC, Bertrand
IPC分类号： A61K31/4025 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4525 , A61K31/4545 , A61K31/46 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K31/4439 , A61P25/28 , A61P9/10 , A61K45/06
CPC分类号： A61K31/4525 , A61K31/4025 , A61K31/4439 , A61K31/453 , A61K31/4535 , A61K31/454 , A61K31/4545 , A61K31/46 , A61K31/506 , A61K31/5377 , A61K31/55 , A61K45/06 , A61K2300/00
摘要： Methods for enhancing cognitive function are disclosed. More particularly, method are disclosed for enhancing cognitive function comprising the step of administerin spirocyclic heterocyclic derivatives (including derivatives of spiro(2H-l-benzopyran-2,4' piperidines) of the general formula (IV):
摘要翻译：公开了增强认知功能的方法。更具体地，公开了用于增强认知功能的方法，其包括施用螺环杂环衍生物（包括通式（IV）的螺（2H-1-苯并吡喃-2,4'哌啶）的衍生物）的步骤：

4. 发明申请

WO2006044645A2 SULFAMOYL BENZAMIDES AND METHODS OF THEIR USE 审中-公开
标题翻译：磺酰苯甲酸及其使用方法
公开(公告)号：WO2006044645A2
公开(公告)日：2006-04-27
申请号：PCT/US2005/036997
申请日：2005-10-12
申请人： ADOLOR CORPORATION , DOLLE, Roland, E. , WORM, Karin , ZHOU, Jean, Q.
发明人： DOLLE, Roland, E. , WORM, Karin , ZHOU, Jean, Q.
IPC分类号： C07D211/06 , A61K31/445
CPC分类号： C07D205/04 , C07C311/16 , C07C311/21 , C07C2602/42 , C07C2603/74 , C07D207/48 , C07D209/44 , C07D211/46 , C07D211/60 , C07D211/96 , C07D213/40 , C07D215/58 , C07D295/26
摘要： Novel sulfamoyl benzamide compounds, pharmaceutical compositions containing the sulfamoyl benzamide compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the sulfamoyl benzamide compounds are agonists and/or modulating ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ischemic conditions, immunerelated disorders, hypertension, neurological disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, for inhibiting mechanical hyperalgesia associated with nerve injury, and as an appetite stimulant.
摘要翻译：公开了新型氨磺酰苯甲酰胺化合物，含有氨磺酰苯甲酰胺化合物的药物组合物及其药物用途的方法。在某些实施方案中，氨磺酰苯甲酰胺化合物是大麻素受体的激动剂和/或调节配体，尤其可用于治疗和/或预防疼痛，胃肠道疾病，炎症，自身免疫疾病，缺血性疾病，免疫反应性疾病，高血压，神经系统疾病和神经变性疾病，用于针对缺血和再灌注作用提供心脏保护，用于诱导恶性细胞凋亡，用于抑制与神经损伤相关的机械性痛觉过敏以及作为食欲刺激剂。

5. 发明申请

WO2007058960A1 SULFAMOYL BENZAMIDES AS CANNABINOID RECEPTOR MODULATORS 审中-公开
标题翻译：磺酰胆碱作为CANNABINOID受体调节剂
公开(公告)号：WO2007058960A1
公开(公告)日：2007-05-24
申请号：PCT/US2006/043846
申请日：2006-11-10
申请人： ADOLOR CORPORATION , DOLLE, Roland, E. , WORM, Karin
发明人： DOLLE, Roland, E. , WORM, Karin
IPC分类号： A61K31/4035 , A61K31/5375 , A61P37/00 , C07D207/12 , C07D209/44 , C07D211/42 , C07D211/44 , C07C311/16 , C07C311/17 , C07C311/19
CPC分类号： C07D295/26 , C07C311/38 , C07C311/40 , C07C311/42 , C07C2601/08 , C07C2601/14 , C07C2602/42 , C07C2603/74 , C07D207/12 , C07D209/44 , C07D211/42 , C07D211/44
摘要： Novel sulfamoyl benzamide compounds, pharmaceutical compositions containing the sulfamoyl benzamide compounds, and methods of their pharmaceutical use are disclosed. In certain embodiments, the sulfamoyl benzamide compounds are agonists and/or ligands of cannabinoid receptors and may be useful, inter alia, for treating and/or preventing pain, gastrointestinal disorders, inflammation, auto-immune diseases, ischemic conditions, immune-related disorders, hypertension, neurological disorders, and neurodegenerative diseases, for providing cardioprotection against ischemic and reperfusion effects, for inducing apoptosis in malignant cells, for inhibiting mechanical hyperalgesia associated with nerve injury, and as an appetite stimulant.
摘要翻译：公开了新型氨磺酰苯甲酰胺化合物，含有氨磺酰苯甲酰胺化合物的药物组合物及其药物用途的方法。在某些实施方案中，氨磺酰苯甲酰胺化合物是大麻素受体的激动剂和/或配体，尤其可用于治疗和/或预防疼痛，胃肠道疾病，炎症，自身免疫疾病，缺血性病症，免疫相关疾病，高血压，神经系统疾病和神经变性疾病，用于提供针对缺血和再灌注作用的心脏保护，用于诱导恶性细胞凋亡，用于抑制与神经损伤相关的机械痛觉过敏以及作为食欲刺激剂。

6. 发明申请

WO2005056011A1 METHODS OF PREVENTING AND TREATING NON-OPIOID INDUCED GASTROINTESTINAL DYSFUNCTION 审中-公开
标题翻译：预防和治疗非阿片样物质诱导胃肠功能障碍的方法
公开(公告)号：WO2005056011A1
公开(公告)日：2005-06-23
申请号：PCT/US2004/039931
申请日：2004-11-30
申请人： ADOLOR CORPORATION , GLAXO GROUP LIMITED , CARPENTER, Randall, L. , DUKES, George, E. , JACKSON, David , SCHMIDT, William, K.
发明人： CARPENTER, Randall, L. , DUKES, George, E. , JACKSON, David , SCHMIDT, William, K.
IPC分类号： A61K31/451
CPC分类号： A61K31/451
摘要： Methods of preventing and treating non-opioid induced gastrointestinal dysfunction, including chronic constipation, slow colonic transit, low stool frequency, and poor stool consistency, with reduced undesirable side effects are disclosed.
摘要翻译：公开了预防和治疗非阿片样物质诱导的胃肠功能障碍的方法，包括慢性便秘，慢结肠转运，低便量和低粪便稠度，减少了不良副作用。

7. 发明申请

WO2005051367A1 CARBOXAMIDE AND AMINO DERIVATIVES AND METHODS OF THEIR USE 审中-公开
标题翻译：羧酰胺和氨基衍生物及其使用方法
公开(公告)号：WO2005051367A1
公开(公告)日：2005-06-09
申请号：PCT/US2004/038656
申请日：2004-11-18
申请人： ADOLOR CORPORATION , DOLLE, Roland, E.
发明人： DOLLE, Roland, E.
IPC分类号： A61K31/00
CPC分类号： C07D401/04 , A61K31/4709 , A61K38/00 , A61K45/06 , C07K5/06008 , C07K5/1013 , C07K5/123 , C07K5/126 , C07K7/56 , C07K7/60
摘要： Carboxamide and amino derivatives, phamaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the carboxamide derivatives are ligands of the δ opioid receptor and are useful, inter alia , for treating and/or preventing pain, anxiety, gastrointestinal disorders, cancer, and other δ opioid receptor-mediated conditions.
摘要翻译：公开了羧酰胺和氨基衍生物，含有这些化合物的药物组合物及其药物用途的方法。在某些实施方案中，羧酰胺衍生物是δ阿片样物质受体的配体，尤其用于治疗和/或预防疼痛，焦虑，胃肠道疾病，癌症和其他δ阿片受体介导的病症。

8. 发明申请

WO2004093796A3 LACTAM DERIVATIVES AND METHODS OF THEIR USE 审中-公开
公开(公告)号：WO2004093796A3
公开(公告)日：2004-11-04
申请号：PCT/US2004/011831
申请日：2004-04-16
申请人： ADOLOR CORPORATION , DOLLE, Roland, E. , TUTHILL, Paul, A.
发明人： DOLLE, Roland, E. , TUTHILL, Paul, A.
IPC分类号： C07D225/02
摘要： Lactam derivatives of the general formula (I), are disclosed. Pharmaceutical compositions containing the compounds and methods for their use are also disclosed.

9. 发明申请

WO2001037785A3 NOVEL METHODS AND COMPOSITIONS INVOLVING OPIOIDS AND ANTAGONISTS THEREOF 审中-公开
公开(公告)号：WO2001037785A3
公开(公告)日：2001-05-31
申请号：PCT/US2000/042315
申请日：2000-11-29
申请人： ADOLOR CORPORATION , FARRAR, John, J.
发明人： FARRAR, John, J.
IPC分类号： A61K31/445
摘要： Novel methods and compositions comprising opioids and opioid antagonists. In preferred embodiments, the methods and compositions comprise opioids and peripheral mu opioid antagonist compounds. The methods and compositions are particularly suitable for treating and/or preventing side effects associated with opioids including, for example, constipation, vomiting and/or nausea. Figures 2A aand 2B are graphical representations of studies on the inhibition of nausea and vomiting employing methods according to an embodiment of the present invention,

10. 发明申请

WO1997032857A1 KAPPA AGONIST COMPOUNDS AND PHARMACEUTICAL FORMULATIONS THEREOF 审中-公开
标题翻译： KAPPA激素化合物及其药物制剂
公开(公告)号：WO1997032857A1
公开(公告)日：1997-09-12
申请号：PCT/US1997003353
申请日：1997-03-01
申请人： ADOLOR CORPORATION , KRUSE, Lawrence, I. , CHANG, An-Chih , DEHAVEN-HUDKINS, Diane, L. , FARRAR, John, J. , GAUL, Forrest , MARELLA, Michael, Anthony , MAYCOCK, Alan, L. , ZHANG, Wei, Yuan
发明人： ADOLOR CORPORATION
IPC分类号： C07D241/04
CPC分类号： C07D295/073 , A61K31/404 , A61K31/4439 , C07D209/42 , C07D213/56 , C07D241/04
摘要： Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formulae (I), (II), (III) and (IV) have the structure wherein X, X4, X5, X7, X9; R1, R2, R3, R4; and Y, Z and n are as described in the specification.
摘要翻译：提供了具有κ阿片样物质激动剂活性的化合物，含有它们的组合物和使用它们作为止痛剂的方法。式（I），（II），（III）和（IV）的化合物具有其中X，X4，X5，X7，X9; R1，R2，R3，R4; Y，Z和n如说明书所述。

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