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1. 发明专利

IL291951A Muscarinic acetylcholine m1 receptor antagonists 未知
公开(公告)号：IL291951A
公开(公告)日：2022-06-01
申请号：IL29195122
申请日：2022-04-04
申请人： PIPELINE THERAPEUTICS INC , BACCEI JILL MELISSA , BRAVO YALDA , CHEN AUSTIN CHIH YU , ROPPE JEFFREY ROGER , SCHRADER THOMAS , XIONG YIFENG
发明人： BACCEI JILL MELISSA , BRAVO YALDA , CHEN AUSTIN CHIH-YU , ROPPE JEFFREY ROGER , SCHRADER THOMAS , XIONG YIFENG
摘要： Provided herein, inter alia, are compounds which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

2. 发明专利

IL291951D0 Muscarinic acetylcholine m1 receptor antagonists 未知
公开(公告)号：IL291951D0
公开(公告)日：2022-06-01
申请号：IL29195122
申请日：2022-04-04
申请人： PIPELINE THERAPEUTICS INC , BACCEI JILL MELISSA , BRAVO YALDA , CHEN AUSTIN CHIH YU , ROPPE JEFFREY ROGER , SCHRADER THOMAS , XIONG YIFENG
发明人： BACCEI JILL MELISSA , BRAVO YALDA , CHEN AUSTIN CHIH-YU , ROPPE JEFFREY ROGER , SCHRADER THOMAS , XIONG YIFENG
IPC分类号： A61P25/00
摘要： Provided herein, inter alia, are compounds which are useful as antagonists of the muscarinic acetylcholine receptor M1 (mAChR M1); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions.

3. 发明申请

WO2007136875A3 ACETAMIDE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：作为用于治疗相关疾病的5-HT2A丝氨酸受体的调节剂的乙酰胺衍生物
公开(公告)号：WO2007136875A3
公开(公告)日：2008-04-10
申请号：PCT/US2007012230
申请日：2007-05-17
申请人： ARENA PHARM INC , TEEGARDEN BRADLEY , FEICHTINGER KONRAD , STRAH-PLEYNET SONJA , ULMANN BRETT , XIONG YIFENG
发明人： TEEGARDEN BRADLEY , FEICHTINGER KONRAD , STRAH-PLEYNET SONJA , ULMANN BRETT , XIONG YIFENG
IPC分类号： C07D413/12 , A61K31/415 , C07D213/12 , C07D401/12 , C07D403/12 , C07D407/14
CPC分类号： C07D231/16 , C07D231/12 , C07D401/12 , C07D405/12 , C07D417/12
摘要： The present invention pertains to certain compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT 2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, blood clot formation, asthma or symptoms thereof, agitation or a symptom thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT 2A serotonin receptor associated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译：本发明涉及某些式（Ia）的化合物及其药物组合物，其调节5-HT 2A 5-羟色胺受体的活性。化合物及其药物组合物涉及可用于治疗血小板凝集，冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，血块形成，哮喘或其症状，躁动或其症状的方法，精神病，精神病，急性精神分裂症，慢性精神分裂症，精神分裂症精神分裂症和相关疾病，睡眠障碍，睡眠障碍，糖尿病性精神病，精神病，精神病，精神病，相关疾病，进行性多灶性脑白质病等。本发明还涉及与单独或一起施用的其它药剂组合治疗5-HT 2A 5-羟色胺受体相关疾病的方法。

4. 发明申请

WO2008054748A3 INDAZOLE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：吲唑衍生物作为5-HT2A血清素受体调节剂，用于治疗与其相关的疾病
公开(公告)号：WO2008054748A3
公开(公告)日：2008-08-07
申请号：PCT/US2007022921
申请日：2007-10-30
申请人： ARENA PHARM INC , FEICHTINGER KONRAD , XIONG YIFENG , CHOI JIN SUN KAROLINE , SMITH BRIAN M , STRAH-PLEYNET SONJA , TEEGARDEN BRADLEY
发明人： XIONG YIFENG , CHOI JIN SUN KAROLINE , SMITH BRIAN M , STRAH-PLEYNET SONJA , TEEGARDEN BRADLEY
IPC分类号： C07D231/56 , A61K31/496 , A61P7/00 , A61P11/00 , A61P25/18 , C07D403/06
CPC分类号： C07D231/56 , C07D403/06
摘要： Indazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the serotonin 5HT 2A receptor. Formula (Ia) Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to the methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译：式（Ia）的吲唑衍生物及其调节血清素5HT2A受体活性的药物组合物。式（Ia）化合物及其药物组合物涉及用于治疗失眠和相关睡眠障碍，血小板聚集，冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房纤颤，降低血液风险的方法激动或其症状，行为障碍，药物诱导的精神病，兴奋性精神病，吉尔斯德拉图雷特综合征，躁狂症，有机或NOS精神病，精神病，精神病，急性精神分裂症，慢性精神分裂症，NOS精神分裂症和相关病症，糖尿病相关病症，进行性多灶性白质脑病等。本发明还涉及与单独或一起施用的其他药剂联合治疗5-HT 2A血清素受体介导的病症的方法。

5. 发明申请

WO2004076413A3 PHENYL- AND PYRIDYLPIPERIDINE-DERIVATIVES AS MODULATORS OF GLUCOSE METABOLISM 审中-公开
标题翻译：作为葡萄糖代谢物的调节剂的苯乙基和吡啶并吡啶衍生物
公开(公告)号：WO2004076413A3
公开(公告)日：2004-12-02
申请号：PCT/US2004005555
申请日：2004-02-23
申请人： ARENA PHARM INC , JONES ROBERT M , SEMPLE GRAEME , CHOI JIN SUN KAROLINE , XIONG YIFENG , FIORAVANTI BEATRIZ
发明人： JONES ROBERT M , SEMPLE GRAEME , CHOI JIN SUN KAROLINE , XIONG YIFENG , FIORAVANTI BEATRIZ
IPC分类号： A61P3/00 , C07D211/14 , C07D211/62 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D413/04 , C07D413/12 , C07D417/14 , A61K31/435
CPC分类号： C07D401/04 , C07D211/14 , C07D211/62 , C07D401/10 , C07D401/12 , C07D401/14 , C07D413/04 , C07D413/12 , C07D417/14
摘要： The present invention relates to certain certain substituted aryl and heteroaryl derivatives as shown in Formula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.
摘要翻译：本发明涉及作为代谢调节剂的式（Ia）所示的某些取代的芳基和杂芳基衍生物。因此，本发明的化合物可用于预防或治疗代谢紊乱及其并发症，例如糖尿病和肥胖症。

6. 发明申请

WO2005121121A3 SUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：作为代谢物和丙肝的调节剂和与之相关的疾病的治疗的替代性ARYL和HETEROARYL衍生物
公开(公告)号：WO2005121121A3
公开(公告)日：2006-03-16
申请号：PCT/US2005019318
申请日：2005-06-02
申请人： ARENA PHARM INC , JONES ROBERT M , SEMPLE GRAEME , XIONG YIFENG , SHIN YOUNG-JUN , REN ALBERT S , LEHMANN JUERG , FIORAVANTI BEATRIZ , BRUCE MARC A , CHOI JIN SUN KAROLINE
发明人： JONES ROBERT M , SEMPLE GRAEME , XIONG YIFENG , SHIN YOUNG-JUN , REN ALBERT S , LEHMANN JUERG , FIORAVANTI BEATRIZ , BRUCE MARC A , CHOI JIN SUN KAROLINE
IPC分类号： C07D401/04 , A61K31/506 , A61P3/10 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
CPC分类号： C07D401/04 , C07D239/48 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The present invention relates to certain substituted aryl and heteroaryl derivative of Formula (I) that are modulators of metabolism, especially of the activity of a GPCR, referred to herein as RUP3. Accordingly, compounds of the present invention are useful in the treatment of metabolic-related disorders and complications thereof, such as, diabetes and obesity.
摘要翻译：本发明涉及作为代谢调节剂（特别是GPCR的活性，称为RUP3）的式（I）的某些取代的芳基和杂芳基衍生物。因此，本发明的化合物可用于治疗代谢相关疾病及其并发症，例如糖尿病和肥胖症。

7. 发明申请

WO2005007647A9 TRISUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PROPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：三取代芳基和杂芳基衍生物作为代谢调节剂和预防和治疗与其相关的疾病
公开(公告)号：WO2005007647A9
公开(公告)日：2005-04-07
申请号：PCT/US2004022327
申请日：2004-07-09
申请人： ARENA PHARM INC , JONES ROBERT M , SEMPLE GRAEME , XIONG YIFENG , SHIN YOUNG-JUN , REN ALBERT S , CALDERON IMELDA , CHOI JIN SUN KAROLINE , FIORAVANTI BEATRIZ , LEHMANN JUERG , BRUCE MARC A
发明人： JONES ROBERT M , SEMPLE GRAEME , XIONG YIFENG , SHIN YOUNG-JUN , REN ALBERT S , CALDERON IMELDA , CHOI JIN SUN KAROLINE , FIORAVANTI BEATRIZ , LEHMANN JUERG , BRUCE MARC A
IPC分类号： A61K31/4439 , A61K31/513 , A61P3/10 , C07D239/52 , C07D239/54 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , A61K31/505 , A61K31/506 , A61K31/5377
CPC分类号： C07D239/52 , C07D239/54 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： The present invention relates to certain trisubstituted aryl and heteroaryl derivatives of Formula (I) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.
摘要翻译：本发明涉及作为代谢调节剂的式（I）的某些三取代的芳基和杂芳基衍生物。因此，本发明化合物可用于预防或治疗代谢紊乱及其并发症，例如糖尿病和肥胖症。

8. 发明申请

WO2004065380A8 1,2,3-TRISUBSTITUTED ARYL AND HETEROARYL DERIVATIVES AS MODULATORS OF METABOLISM AND THE PRPPHYLAXIS AND TREATMENT OF DISORDERS RELATED THERETO SUCH AS DIABETES AND HYPERGLYCEMIA 审中-公开
标题翻译：作为代谢物和抑制剂的调节剂和治疗与糖尿病和高血压相关的疾病的1,2-三取代的芳基和异构体衍生物
公开(公告)号：WO2004065380A8
公开(公告)日：2004-10-21
申请号：PCT/US2004001267
申请日：2004-01-14
申请人： ARENA PHARM INC , JONES ROBERT M , SEMPLE GRAEME , FIORAVANTI BEATRIZ , PEREIRA GUILHERME , CALDERON IMELDA , UY JANE , DUVVURI KAMESHWARI , CHOI JIN SUN KAROLINE , XIONG YIFENG , DAVE VIBHA
发明人： JONES ROBERT M , SEMPLE GRAEME , FIORAVANTI BEATRIZ , PEREIRA GUILHERME , CALDERON IMELDA , UY JANE , DUVVURI KAMESHWARI , CHOI JIN SUN KAROLINE , XIONG YIFENG , DAVE VIBHA
IPC分类号： A61K31/513 , A61P3/10 , C07D213/68 , C07D213/79 , C07D239/34 , C07D239/50 , C07D295/096 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D411/14 , C07D413/14 , C07D417/14 , C07D419/14
CPC分类号： C07D213/68 , C07D213/79 , C07D239/34 , C07D239/50 , C07D295/096 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D411/14 , C07D413/14 , C07D417/14 , C07D419/14
摘要： The present invention relates to certain 1,2,3-trisubstituted aryl and heteroaryl derivatives of Fomula (Ia) that are modulators of metabolism. Accordingly, compounds of the present invention are useful in the prophylaxis or treatment of metabolic disorders and complications thereof, such as, diabetes and obesity.
摘要翻译：本发明涉及作为代谢调节剂的Fomula（Ia）的某些1,2,3-三取代的芳基和杂芳基衍生物。因此，本发明的化合物可用于预防或治疗代谢紊乱及其并发症，例如糖尿病和肥胖症。

9. 发明申请

WO2004027388A3 NOVEL GREEN AND ORANGE FLUORESCENT LABELS AND THEIR USES 审中-公开
标题翻译：新的绿色和橙色荧光标签及其用途
公开(公告)号：WO2004027388A3
公开(公告)日：2004-06-10
申请号：PCT/US0330167
申请日：2003-09-23
申请人： CHROMAGEN INC , BHATT RAM , CONRAD MICHAEL J , BENCHEIKH AZZOUZ , XIONG YIFENG
发明人： BHATT RAM , CONRAD MICHAEL J , BENCHEIKH AZZOUZ , XIONG YIFENG
IPC分类号： C07C309/50 , C07C309/51 , C07C311/29 , C07C331/20 , C07D207/44 , C07D207/452 , C07D207/46 , G01N33/533 , C07C309/63 , A61K31/10
CPC分类号： C07D207/46 , C07C309/50 , C07C309/51 , C07C311/29 , C07C331/20 , C07C2603/50 , C07D207/452 , G01N33/533 , Y10S436/80
摘要： The present invention provides novel fluorescent compounds and covalent attachment chemistries which facilitate the use of these compounds as labels for ultrasensitive and quantitative fluorescent detection of low levels of biomolecules. In a preferred embodiment, the fluorescent labels of this invention are novel derivatives of the hydroxy-pyrene trisulphonic and disulphonic acids which may be used in any assay in which radioisotopes, colored dyes or other fluorescent molecules are currently used. Thus, for example, any assay using labeled antibodies, proteins, oligonucleotides or lipids, including fluorescent cell sorting, fluorescence microscopy (including dark-field microscopy), fluorescence polarization assays, ligand, receptor binding assays, receptor activation assays and diagnostic assays can benefit from use of the compounds disclosed herein.
摘要翻译：本发明提供了新颖的荧光化合物和共价连接化学物质，其有利于使用这些化合物作为标记用于超低灵敏度和定量荧光检测低水平生物分子。在一个优选的实施方案中，本发明的荧光标记是羟基芘三磺酸和二磺酸的新衍生物，其可用于任何其中目前使用放射性同位素，有色染料或其他荧光分子的测定中。因此，例如，使用标记抗体，蛋白质，寡核苷酸或脂质（包括荧光细胞分选，荧光显微术（包括暗视野显微术），荧光偏振测定，配体，受体结合测定，受体活化测定和诊断测定）的任何测定可以受益从使用本文公开的化合物。

10. 发明申请

WO2009023253A3 IMIDAZO[L,2-a]PYRIDINE DERIVATIVES AS MODULATORS OF THE 5-HT2A SEROTONIN RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：作为用于治疗相关疾病的5-HT2A丝氨酸受体的调节剂的咪唑并[L，2-a]吡啶衍生物
公开(公告)号：WO2009023253A3
公开(公告)日：2009-04-09
申请号：PCT/US2008009740
申请日：2008-08-14
申请人： ARENA PHARM INC , XIONG YIFENG , FEICHTINGER KONRAD , REN ALBERT S , ULMANN BRETT
发明人： XIONG YIFENG , FEICHTINGER KONRAD , REN ALBERT S , ULMANN BRETT
IPC分类号： C07D471/04 , A61K31/437 , A61P25/20
CPC分类号： A61K31/496 , A61K9/0019 , A61K9/0053 , A61K31/5377 , C07D471/04
摘要： rmidazo[l,2-a]pyridine derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of insomnia, dyssomnia, parasomnia and related sleep disorders, platelet aggregation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, thrombosis, asthma or symptoms thereof, agitation or symptoms thereof, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de Ia Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorders, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, diabetic- related disorders, progressive multifocal leukoencephalopathy and the like. The present invention also relates to methods for the treatment of 5-HT2A serotonin receptor mediated disorders in combination with other pharmaceutical agents administered separately or together.
摘要翻译：式（Ia）的咪唑并[1,2-a]吡啶衍生物及其药物组合物，其调节5-HT2A 5-羟色胺受体的活性。化合物及其药物组合物涉及可用于治疗失眠，睡眠不良，失眠和相关睡眠障碍，血小板聚集，冠状动脉疾病，心肌梗塞，短暂性脑缺血发作，心绞痛，中风，心房颤动，血栓形成，哮喘或症状的方法糖尿病，糖尿病，精神病，精神病，精神分裂症，慢性精神分裂症，精神分裂症，精神分裂症，糖尿病，糖尿病，糖尿病，糖尿病，糖尿病，糖尿病，糖尿病，糖尿病，相关疾病，进行性多灶性脑白质病等。本发明还涉及与单独或一起施用的其它药剂组合治疗5-HT2A 5-羟色胺受体介导的病症的方法。

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