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31. 发明授权

US08637555B2 Tetrazole derivatives and methods of treatment of metabolic-related disorders thereof 失效
标题翻译：四唑衍生物及其代谢相关病症的治疗方法
公开(公告)号：US08637555B2
公开(公告)日：2014-01-28
申请号：US10535345
申请日：2004-10-29
申请人： Graeme Semple , Thomas Schrader , Philip J. Skinner , Steven L. Colletti , Tawfik Gharbaoui , Jason E. Imbriglio , Jae-Kyu Jung , Rui Liang , Subharekha Raghavan , Darby Schmidt , James R. Tata
发明人： Graeme Semple , Thomas Schrader , Philip J. Skinner , Steven L. Colletti , Tawfik Gharbaoui , Jason E. Imbriglio , Jae-Kyu Jung , Rui Liang , Subharekha Raghavan , Darby Schmidt , James R. Tata
IPC分类号： A61K31/407 , C07D231/54
CPC分类号： C07D491/04 , C07D403/04 , C07D495/04
摘要： The present invention relates to certain tetrazole derivatives of Formula (I), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers and the like.
摘要翻译：本发明涉及式（I）的某些四唑衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为RUP25受体的激动剂。本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病，综合征-X等。此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂等。

32. 发明授权

US07241792B2 Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof 有权
标题翻译：融合的吡唑衍生物及其代谢相关病症的治疗方法
公开(公告)号：US07241792B2
公开(公告)日：2007-07-10
申请号：US11315753
申请日：2005-12-22
申请人： P. Douglas Boatman , Thomas O. Schrader , Graeme Semple , Philip J. Skinner , Jae-Kyu Jung
发明人： P. Douglas Boatman , Thomas O. Schrader , Graeme Semple , Philip J. Skinner , Jae-Kyu Jung
IPC分类号： A61K31/407 , C07D231/54
CPC分类号： C07D403/04 , C07D209/80 , C07D209/88 , C07D231/54 , C07D265/36 , C07D471/04 , C07D471/14
摘要： The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.
摘要翻译：本发明涉及式（Ia）的某些稠合吡唑衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为RUP25受体的激动剂。本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病的方法，综合征-X等。此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂，DP受体拮抗剂等。

33. 发明授权

US07176195B2 Fused azepine derivatives and their use as antidiuretic agents 失效
标题翻译：稠合的吖庚因衍生物及其作为抗利尿剂的用途
公开(公告)号：US07176195B2
公开(公告)日：2007-02-13
申请号：US10311301
申请日：2001-06-21
申请人： Doreen Ashworth , Gary R. W. Pitt , Peter Hudson , Christopher Yea , Richard J. Franklin , Graeme Semple , David Paul Jenkins
发明人： Doreen Ashworth , Gary R. W. Pitt , Peter Hudson , Christopher Yea , Richard J. Franklin , Graeme Semple , David Paul Jenkins
IPC分类号： A61P7/12 , A61K31/55 , C07D487/00 , C07D498/00 , C07D513/00
CPC分类号： C07D223/16 , C07D243/12 , C07D267/14 , C07D281/10 , C07D401/06 , C07D401/12 , C07D403/12 , C07D413/12 , C07D471/04 , C07D487/04 , C07D495/04
摘要： Compounds according to general formulae (1 and 2), wherein G1 is an azepine derivative and G2 is a group according to general formulae (9–11) are new. Compounds according to the invention are vasopressin V2 receptor agonists. Pharmaceutical compositions of the compounds are useful as antidiuretic agents
摘要翻译：根据通式（1和2）的化合物，其中G 1是吖庚因衍生物，而G 2是根据通式（9-11）的基团。根据本发明的化合物是加压素V 2 O 2受体激动剂。化合物的药物组合物可用作抗利尿剂

34. 发明授权

US06214798B1 GnRH antagonists being modified in positions 5 and 6 有权
标题翻译： GnRH拮抗剂在5和6位修饰
公开(公告)号：US06214798B1
公开(公告)日：2001-04-10
申请号：US09402698
申请日：2000-01-03
申请人： Graeme Semple , Guangcheng Jiang
发明人： Graeme Semple , Guangcheng Jiang
IPC分类号： A61K3800
CPC分类号： C07K7/23 , A61K38/00 , Y02P20/55 , Y10S514/80 , Y10S930/11
摘要： Peptides are provided which have improved duration of GnRH antagonistic properties. These antagonists may be used to regulate fertility and to treat steroid-dependent tumors and for other short-term and long-term treatment indications. These antagonists have a derivative of aminoPhe or its equivalent in the 5- or the 5- and 6-positions. This derivative is modified so as to contain a carbamoyl group or heterocycle, including a urea moiety, in its side chain. Decapeptides having the formula: Ac-D-2Nal-D-4Cpa-D-3Pal-Ser-4Aph(L-hydroorotyl)-D-4Amf(Q2)-Leu-Lys(isopropyl)-Pro-Xaa10, wherein Q2 is Cbm or MeCbm and Xaa10 is D-Ala-ol or Ala-ol are particularly effective and continue to exhibit very substantial suppression of LH secretion at 96 hours following injection.
摘要翻译：提供具有改善的GnRH拮抗性能持续时间的肽。这些拮抗剂可用于调节生育力和治疗类固醇依赖性肿瘤和其他短期和长期治疗适应症。这些拮抗剂在5-或5-和6-位具有氨基Phe的衍生物或其等同物。该衍生物被修饰为在其侧链中含有氨基甲酰基或杂环，包括脲部分。具有下式的十肽：其中Q2是Cbm或MeCbm，Xaa10是D-Ala-ol或Ala-ol是特别有效的，并且在注射后96小时继续表现出非常实质的LH分泌抑制。

35. 发明授权

US5962451A Benzodiazepin derivatives useful as CCK-receptor antagonists 失效
标题翻译：苯并二氮杂衍生物可用作CCK受体拮抗剂
公开(公告)号：US5962451A
公开(公告)日：1999-10-05
申请号：US867422
申请日：1997-06-06
申请人： Hamish Ryder , Graeme Semple , David Alan Kendrick , Michael Szelke , Masato Satoh , Mitsuaki Ohta , Keiji Miyata , Akito Nishida
发明人： Hamish Ryder , Graeme Semple , David Alan Kendrick , Michael Szelke , Masato Satoh , Mitsuaki Ohta , Keiji Miyata , Akito Nishida
IPC分类号： A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/55 , A61K31/551 , A61K31/5513 , A61P1/04 , A61P25/00 , A61P43/00 , C07D243/24 , C07D243/34 , C07D401/04 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D243/10
CPC分类号： C07D401/04 , C07D243/24 , C07D403/06
摘要： A benzodiazepine derivative of formula (I), or a pharmaceutically acceptable salt thereof, wherein (a) R.sup.1 is --CH.sub.2 CHOH(CH.sub.2).sub.a R.sup.4 or a ketone group --CH.sub.2 CO(CH.sub.2).sub.a R.sup.5 in which a is 0 or 1 and R.sup.4 and R.sup.5 are selected from alkyl and cycloalkyl groups and saturated heterocyclic groups optionally substituted at a hetero-atom; (b) R.sup.2 and R.sup.3 are independently selected from aromatic carbocyclic and heterocylic residues; and (c) W and X are selected independently from halogen and hydrogen atoms and alkyl and alkoxy groups. These compounds are gastrin and/or CCK-B receptor antagonists. ##STR1##
摘要翻译：式（I）的苯并二氮杂衍生物或其药学上可接受的盐，其中（a）R 1为-CH 2 CHOH（CH 2）aR 4或酮基-CH 2 CO（CH 2）a R 5，其中a为0或1，且R 4和R 5为选自烷基和环烷基和任选在杂原子处被取代的饱和杂环基; （b）R2和R3独立地选自芳族碳环和杂环残基; 和（c）W和X独立地选自卤素和氢原子以及烷基和烷氧基。这些化合物是胃泌素和/或CCK-B受体拮抗剂。

36. 发明申请

US20100240653A1 BIPHENYL SULFONYL AND PHENYL-HETEROARYL SULFONYL MODULATORS OF THE HISTAMINE H3-RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO 审中-公开
标题翻译：用于治疗相关疾病的组胺H3受体的联苯磺隆和苯并噻吩磺酸盐调节剂
公开(公告)号：US20100240653A1
公开(公告)日：2010-09-23
申请号：US12445795
申请日：2007-10-16
申请人： Vincent J. Santora , Ryan M. Hart , Jason B. Ibarra , Douglas M. Park , Albert S. Ren , Graeme Semple , Jeffrey A. Schultz , Brian M. Smith , Jeffrey Smith
发明人： Vincent J. Santora , Ryan M. Hart , Jason B. Ibarra , Douglas M. Park , Albert S. Ren , Graeme Semple , Jeffrey A. Schultz , Brian M. Smith , Jeffrey Smith
IPC分类号： A61K31/4025 , A61K31/5377 , A61K31/506 , A61K31/454 , A61K31/4439 , A61K31/40 , C07D413/12 , C07D403/10 , C07D401/12 , C07D401/10 , C07D409/10 , C07D207/06 , A61P25/28 , C07D405/10 , A61P25/00 , A61P25/24 , A61P3/04 , A61P25/18 , A61P37/08 , A61P11/00
CPC分类号： C07D207/06 , C07D401/12 , C07D403/10 , C07D405/12 , C07D409/10 , C07D417/10
摘要： The present invention relates to certain biphenyl sulfonamide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3-receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as, cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as narcolepsy, shift-work syndrome, drowsiness as a side effect from a medication, maintenance of vigilance to aid in completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease and the like.
摘要翻译：本发明涉及式（Ia）的某些联苯磺酰胺衍生物及其药物组合物，其调节组胺H3受体的活性。本发明的化合物及其药物组合物涉及可用于治疗组胺H3相关疾病例如认知障碍，癫痫，脑外伤，抑郁症，肥胖症，睡眠障碍和觉醒症如发作性睡眠，工作综合征，作为药物副作用的睡意，维持警惕以完成任务等，猝倒，睡眠过多，嗜睡症，时差，睡眠呼吸暂停等，注意力缺陷多动障碍（ADHD），精神分裂症过敏，上呼吸道过敏反应，过敏性鼻炎，鼻塞，痴呆，阿尔茨海默氏病等。

37. 发明授权

US07612106B2 Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof 有权
标题翻译：融合的吡唑衍生物及其代谢相关病症的治疗方法
公开(公告)号：US07612106B2
公开(公告)日：2009-11-03
申请号：US11601184
申请日：2006-11-17
申请人： P. Douglas Boatman , Thomas O. Schrader , Graeme Semple , Philip J. Skinner , Jae-Kyu Jung
发明人： P. Douglas Boatman , Thomas O. Schrader , Graeme Semple , Philip J. Skinner , Jae-Kyu Jung
IPC分类号： A61K31/407 , C07D231/54
CPC分类号： C07D403/04 , C07D209/80 , C07D209/88 , C07D231/54 , C07D265/36 , C07D471/04 , C07D471/14
摘要： The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.
摘要翻译：本发明涉及式（Ia）的某些稠合吡唑衍生物及其药学上可接受的盐，其表现出有用的药理学性质，例如作为RUP25受体的激动剂。本发明还提供含有本发明化合物的药物组合物，以及使用本发明化合物和组合物治疗代谢相关疾病包括血脂异常，动脉粥样硬化，冠心病，胰岛素抵抗，2型糖尿病的方法，综合征-X等。此外，本发明还提供本发明化合物与其它活性剂如属于α-葡糖苷酶抑制剂类，醛糖还原酶抑制剂，双胍类，HMG-CoA还原酶抑制剂，角鲨烯合成抑制剂，贝特类，LDL分解代谢增强剂，血管紧张素转换酶（ACE）抑制剂，胰岛素分泌增强剂，DP受体拮抗剂等。

38. 发明申请

US20090036448A1 PYRIMIDINE DERIVATIVES AND METHODS OF TREATMENT RELATED TO THE USE THEREOF 审中-公开
标题翻译：吡嗪衍生物及其使用相关的治疗方法
公开(公告)号：US20090036448A1
公开(公告)日：2009-02-05
申请号：US10599505
申请日：2005-03-29
申请人： Yoshinori Sekiguchi , Kosuke Kanuma , Katsunori Omodera , Thuy-Anh Tran , Graeme Semple , Bryan A. Kramer
发明人： Yoshinori Sekiguchi , Kosuke Kanuma , Katsunori Omodera , Thuy-Anh Tran , Graeme Semple , Bryan A. Kramer
IPC分类号： A61K31/506 , C07D239/48 , A61K31/5377 , A61P3/04 , C07D413/02
CPC分类号： C07D239/42 , C07D239/48 , C07D239/545 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D473/34 , C07D487/04
摘要： The present invention encompasses novel substituted pyrimidine compounds of Formula (I): which act as MCH receptor antagonists. These compounds are useful in pharmaceutical compositions whose use includes prophylaxis or treatment of improving memory function, sleeping and arousal, anxiety, depression, mood disorders, seizure, obesity, diabetes, appetite and eating disorders, cardiovascular disease, hypertension, dyslipidemia, myocardial infarction, binge eating disorders including bulimia, anorexia, mental disorders including manic depression, schizophrenia, delirium, dementia, stress, cognitive disorders, attention deficit disorder, substance abuse disorders and dyskinesias including Parkinson's disease, epilepsy, and addiction.
摘要翻译：本发明包括式（I）的新型取代嘧啶化合物：其作为MCH受体拮抗剂。这些化合物可用于药物组合物，其用途包括预防或治疗改善记忆功能，睡眠和觉醒，焦虑，抑郁，情绪障碍，癫痫发作，肥胖症，糖尿病，食欲和进食障碍，心血管疾病，高血压，血脂异常，心肌梗死，包括贪食症，厌食症，包括躁狂抑郁症，精神分裂症，del妄，痴呆，压力，认知障碍，注意力缺陷障碍，药物滥用障碍和包括帕金森氏病，癫痫和成瘾在内的运动障碍的暴饮暴食症。

39. 发明申请

US20070093545A1 4-Oxo-4,5-dihydro-furan-2-carboxylic acid derivatives and methods of treatment of metabolic-related disorders thereof 审中-公开
标题翻译： 4-氧代-4,5-二氢 - 呋喃-2-羧酸衍生物及其代谢相关病症的治疗方法
公开(公告)号：US20070093545A1
公开(公告)日：2007-04-26
申请号：US10578732
申请日：2004-11-18
申请人： Jae-Kyu Jung , Graeme Semple , Benjamin Johnson
发明人： Jae-Kyu Jung , Graeme Semple , Benjamin Johnson
IPC分类号： A61K31/381 , A61K31/34 , C07D409/02
CPC分类号： C07D307/68 , C07D405/04 , C07D409/04 , C07D409/10
摘要： System for selecting a colour shade comprising a very small number of colour display cards with mixed shades of two or more colours. The system comprises means for selecting one shade among mixed shades, means for presenting the selected mixed shade as well as means for specifying the selected mixed shade for making paint in the desired colour tone.
摘要翻译：用于选择颜色的系统，其包括具有两种或更多种颜色的混合色调的非常少量的彩色显示卡。该系统包括用于选择混合色调中的一个色调的装置，用于呈现所选择的混合色调的装置以及用于指定所选择的混合色调以用于制作所需色调的油漆的装置。

40. 发明申请

US20070073062A1 Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof 有权
公开(公告)号：US20070073062A1
公开(公告)日：2007-03-29
申请号：US11601184
申请日：2006-11-17
申请人： P. Boatman , Thomas Schrader , Graeme Semple , Philip Skinner , Jae-Kyu Jung
发明人： P. Boatman , Thomas Schrader , Graeme Semple , Philip Skinner , Jae-Kyu Jung
IPC分类号： C07D231/54 , C07D403/02
CPC分类号： C07D403/04 , C07D209/80 , C07D209/88 , C07D231/54 , C07D265/36 , C07D471/04 , C07D471/14
摘要： The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.

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