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1.发明授权Carbonate intermediates for the synthesis of purine substituted cyclopentene derivatives 失效用于合成嘌呤取代环戊烯衍生物的碳酸酯中间体
公开(公告)号：US5241069A
公开(公告)日：1993-08-31
申请号：US788667
申请日：1991-11-06
IPC分类号： C07C69/96 , C07D473/18 , C07D473/40
CPC分类号： C07D473/40 , C07C69/96 , C07D473/18
摘要： This invention relates to the new process for preparing the 1R-cis isomer of carbovir, (1R-cis)-amino-1,9-dihydro-9-[4-(hydroxymethyl)-2-cyclopenten-1-yl]-6H-purin-6-one, an antiviral agent and intermediates of the formula (Vlb) use in that process ##STR1## wherein X is chloro, bromo or iodo and R is (C.sub.1-6) alkyl.
摘要翻译： 本发明涉及制备碳水化合物的1R-顺式异构体的新方法，（1R-顺式） - 氨基-1,9-二氢-9- [4-（羟基甲基）-2-环戊烯-1-基] -6H - 嘌呤-6-酮，抗病毒剂和式（VIb）中间体用于该方法（VIb），其中X是氯，溴或碘，R是（C 1-6）烷基。
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公开(公告)号：US5126452A
公开(公告)日：1992-06-30
申请号：US505809
申请日：1990-04-06
IPC分类号： C07C69/96 , C07D473/18 , C07D473/40
CPC分类号： C07D473/40 , C07C69/96 , C07D473/18
摘要： This invention relates to new process for preparing certain optically active purine substituted cyclopentene derivatives and novel intermediates used in this process. In particular, the invention concerns the synthesis of the 1R-cis isomer of carbovir, (1R-cis)-amino-1,9-dihydro-9-[4-(hydroxymethyl)-2-cyclopenten-1-yl]-6H-purin-6-one, an antiviral agent, and certain intermediates.
摘要翻译： 本发明涉及制备某些光学活性嘌呤取代的环戊烯衍生物的新方法和用于该方法的新型中间体。 特别地，本发明涉及羰基维生素的1R-顺式异构体的合成，（1R-顺式） - 氨基-1,9-二氢-9- [4-（羟基甲基）-2-环戊烯-1-基] -6H - 嘌呤-6-酮，抗病毒剂和某些中间体。
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3.发明授权Methods of using macrocyclic agonists of the ghrelin receptor for treatment of gastrointestinal motility disorders 有权使用生长素释放肽受体的大环激动剂治疗胃肠动力障碍的方法公开(公告)号：US08088733B2
公开(公告)日：2012-01-03
申请号：US11774185
申请日：2007-07-06
CPC分类号： A61K31/33
摘要： The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective agonists of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Such compounds are useful as medicaments for treatment and prevention of a range of medical conditions characterized by disturbed gastrointestinal motility including, but not limited to, post-surgical gastroparesis and post-operative ileus in combination with opioid-induced bowel dysfunction. These agents are effective for multiple disorders at dose levels equivalent to those required to treat a single disorder.
摘要翻译： 本发明提供已被证明是生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，同种型及其变体）的选择性激动剂的新的构象定义的大环化合物。 这些化合物可用作治疗和预防特征为紊乱的胃肠蠕动的一系列医学病症的药物，包括但不限于手术后胃轻瘫和与阿片样物质诱导的肠功能障碍联合的术后肠梗阻。 这些药剂对于与治疗单一病症所需的剂量水平相当的剂量水平对多种疾病有效。
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公开(公告)号：US07491695B2
公开(公告)日：2009-02-17
申请号：US11149512
申请日：2005-06-10
CPC分类号： C07K5/0827 , A61K31/395 , A61K31/4545 , A61K31/55 , A61K38/06 , A61K38/12 , C07K5/0808 , C07K5/0812 , Y02A50/395
摘要： The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
摘要翻译： 本发明提供已被证明是生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，同种型及其变体）的选择性调节剂的新型构象定义的大环化合物。 本文还描述了合成新化合物的方法。 这些化合物可用作生长素释放肽受体的激动剂，并且用作治疗和预防一系列医学病症的药物，包括但不限于代谢和/或内分泌疾病，胃肠道疾病，心血管疾病，肥胖症和肥胖相关疾病， 中枢神经系统疾病，遗传疾病，过度增殖性疾病和炎症性疾病。
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5.发明授权Electronic coupon storage and retrieval system correlated to highway exit service availability information 失效电子优惠券存储和检索系统与公路出口服务可用性信息相关
公开(公告)号：US5943653A
公开(公告)日：1999-08-24
申请号：US612344
申请日：1996-03-07
申请人： Monte Ross , Mark L. Peterson , Leonard R. Missler
发明人： Monte Ross , Mark L. Peterson , Leonard R. Missler
CPC分类号： G06Q30/02 , G06Q10/02 , G06Q10/025 , G06Q30/0235 , G06Q30/0238
摘要： A system for providing data related to discounted services available near a given location. The system includes a memory storing compressed service data representative of a plurality of services in various locations categorized by type of service and compressed coupon data representative of discounts available for the services. The system also includes a book of coupons corresponding to the discounted services wherein the coupon data includes identifying numbers which identify locations of coupons within the coupon book corresponding to the discounts available for the services. A data entry circuit receives and compresses input data identifying a desired category of services and the given location and a microprocessor, receiving and responsive to the compressed input data, selectively retrieves the service data and coupon data from the memory. The retrieved service data represents one or more selected services in the desired category near the given location and the retrieved coupon data represents the discounts available for the selected services including the identifying numbers of the coupons. The microprocessor then expands the retrieved service data and coupon data into a user-readable form and a display displays the expanded retrieved service data and coupon data.
摘要翻译： 用于提供与给定位置附近可用的折扣服务有关的数据的系统。 该系统包括存储压缩服务数据的存储器，该压缩服务数据代表根据服务类型分类的各种位置中的多个服务，以及代表可用于服务的折扣的压缩优惠券数据。 该系统还包括与优惠服务相对应的优惠券簿，其中优惠券数据包括标识号码，其识别优惠券内的与可用于服务的折扣相对应的优惠券的位置。 数据输入电路接收并压缩识别期望类别的服务和给定位置的输入数据，并且接收并响应于压缩输入数据的微处理器选择性地从存储器检索服务数据和优惠券数据。 所检索的服务数据表示在给定位置附近的期望类别中的一个或多个所选择的服务，并且所检索的优惠券数据表示可用于所选择的服务的折扣，包括优惠券的识别号码。 然后，微处理器将检索的服务数据和优惠券数据扩展成用户可读的形式，并且显示器显示扩展的检索到的服务数据和优惠券数据。
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6.发明授权Methods of treating cachexia with macrocyclic modulators of the ghrelin receptor 有权用生长素释放肽受体的大环调节剂治疗恶病质的方法公开(公告)号：US08349887B2
公开(公告)日：2013-01-08
申请号：US13173929
申请日：2011-06-30
IPC分类号： A01N43/02
CPC分类号： C07K5/0827 , A61K31/395 , A61K31/4545 , A61K31/55 , A61K38/06 , A61K38/12 , C07K5/0808 , C07K5/0812 , Y02A50/395
摘要： The present invention provides novel conformationally-defined macrocyclic compounds that have been demonstrated to be selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
摘要翻译： 本发明提供已被证明是生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，同种型及其变体）的选择性调节剂的新型构象定义的大环化合物。 本文还描述了合成新化合物的方法。 这些化合物可用作生长素释放肽受体的激动剂，并且用作治疗和预防一系列医学病症的药物，包括但不限于代谢和/或内分泌疾病，胃肠道疾病，心血管疾病，肥胖症和肥胖相关疾病， 中枢神经系统疾病，遗传疾病，过度增殖性疾病和炎症性疾病。
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公开(公告)号：US20110245459A1
公开(公告)日：2011-10-06
申请号：US13036484
申请日：2011-02-28
申请人： Éric Marsault , Kamel Benakli , Hamid R. Hoveyda , Mark L. Peterson , Sylvie Beaubien , Luc Ouellet , Carl St-Louis , Sophie Beauchemin
发明人： Éric Marsault , Kamel Benakli , Hamid R. Hoveyda , Mark L. Peterson , Sylvie Beaubien , Luc Ouellet , Carl St-Louis , Sophie Beauchemin
IPC分类号： C07K5/12
CPC分类号： C07C213/08 , A61K38/12 , A61K38/2214 , C07C41/18 , C07C67/343 , C07D273/00 , C07D413/06 , C07D498/04 , C07K5/0812 , C07K5/0821 , C07K5/0827
摘要： The present invention is directed to novel macrocyclic compounds of formula (I) and their pharmaceutically acceptable salts, hydrates or solvates: wherein R1, R2, R3, R4, R5, R6, n1, m, p Z1, Z2, and Z3 are as describe in the specification. The invention also relates to compounds of formula (I) which are antagonists of the motilin receptor and are useful in the treatment of disorders associated with this receptor and with or with motility dysfunction.
摘要翻译： 本发明涉及式（I）的新型大环化合物及其药学上可接受的盐，水合物或溶剂化物：其中R1，R2，R3，R4，R5，R6，n1，m，pZ1，Z2和Z3为 在规范中描述。 本发明还涉及作为胃动素受体的拮抗剂的式（I）化合物，并且可用于治疗与该受体相关并伴有或具有运动功能障碍的病症。
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公开(公告)号：US5229947A
公开(公告)日：1993-07-20
申请号：US676818
申请日：1991-03-28
申请人： Monte Ross , Mark L. Peterson , Leonard R. Missler
发明人： Monte Ross , Mark L. Peterson , Leonard R. Missler
IPC分类号： G09B29/10
CPC分类号： G09B29/106
摘要： A data processing device for providing data related to the categories of services available at locations along a highway in response to operator input is disclosed. The device includes a memory, a keyboard for entering input data identifying a desired service and an origin position into the memory. The input data is compressed before it is stored in the memory. The memory stores predetermined data in a compressed form related to the categories of services available at locations along the highway. The device also includes a microprocessor for retrieving from the memory the predetermined data which is a function of the input data. The microprocessor expands the retrieved compressed data into an operator readable form and provides the expanded data to a display for displaying the expanded retrieved data such as restaurants, gas stations, motels, or other services along the highway.
摘要翻译： 公开了一种数据处理装置，用于响应于操作者输入提供与沿着高速公路的位置可用的服务类别相关的数据。 该装置包括存储器，用于输入识别期望服务的输入数据的键盘和存储器中的原始位置。 输入数据在存储在存储器中之前被压缩。 存储器以与沿着高速公路的位置可用的服务类别相关的压缩形式存储预定数据。 该装置还包括微处理器，用于从存储器检索作为输入数据的函数的预定数据。 微处理器将所检索的压缩数据扩展为操作者可读形式，并将扩展数据提供给显示器，以显示沿着公路的扩展的检索数据，例如餐馆，加油站，汽车旅馆或其他服务。
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公开(公告)号：US5021961A
公开(公告)日：1991-06-04
申请号：US410603
申请日：1989-09-21
申请人： Monte Ross , Mark L. Peterson , Leonard R. Missler
发明人： Monte Ross , Mark L. Peterson , Leonard R. Missler
IPC分类号： G09B29/10
CPC分类号： G09B29/106
摘要： A data processing device for providing data related to the categories of services available at locations along a highway in response to operator input is disclosed. The device includes a memory, a keyboard for entering input data identifying a desired service and an origin position into the memory. The input data is compressed before it is stored in the memory. The memory stores predetermined data in a compressed form related to the categories of services available at locations along the highway. The device also includes a microprocessor for retrieving from the memory the predetermined data which is a function of the input data. The microprocessor expands the retrieved compressed data into an operator readable form and provides the expanded data to a display for displaying the expanded retrieved data such as restaurants, gas stations, motels, or other services along the highway.
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10.发明授权公开(公告)号：US09371297B2
公开(公告)日：2016-06-21
申请号：US12028611
申请日：2008-02-08
申请人： Hamid Hoveyda , Graeme L. Fraser , Kamel Benakli , Sophie Beauchemin , Martin Brassard , Eric Marsault , Luc Oullet , Mark L. Peterson , Zhigang Wang
发明人： Hamid Hoveyda , Graeme L. Fraser , Kamel Benakli , Sophie Beauchemin , Martin Brassard , Eric Marsault , Luc Oullet , Mark L. Peterson , Zhigang Wang
IPC分类号： C07K5/12 , C07D273/00 , C07C271/16 , C07C215/42 , C07C215/54 , C07D413/06 , C07D498/04 , C07D498/16
CPC分类号： A61K31/395 , C07C215/42 , C07C215/54 , C07C271/16 , C07C2601/14 , C07D273/00 , C07D413/06 , C07D498/04 , C07D498/16
摘要： The present invention provides novel conformationally-defined macrocyclic compounds that can function as selective modulators of the ghrelin receptor (growth hormone secretagogue receptor, GHS-R1a and subtypes, isoforms and variants thereof). Methods of synthesizing the novel compounds are also described herein. These compounds are useful as agonists of the ghrelin receptor and as medicaments for treatment and prevention of a range of medical conditions including, but not limited to, metabolic and/or endocrine disorders, gastrointestinal disorders, cardiovascular disorders, obesity and obesity-associated disorders, central nervous system disorders, bone disorders, genetic disorders, hyperproliferative disorders and inflammatory disorders.
摘要翻译： 本发明提供新的构象定义的大环化合物，其可以作为生长素释放肽受体（生长激素促分泌素受体，GHS-R1a和亚型，同种型及其变体）的选择性调节剂。 本文还描述了合成新化合物的方法。 这些化合物可用作生长素释放肽受体的激动剂，并且用作治疗和预防一系列医学病症的药物，包括但不限于代谢和/或内分泌疾病，胃肠道疾病，心血管疾病，肥胖症和肥胖相关疾病， 中枢神经系统疾病，骨骼疾病，遗传疾病，过度增殖性疾病和炎症性疾病。
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