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1. 发明授权

US5597915A Benzodiazepine derivatives, compositions containing them and their use in therapy 失效
标题翻译：苯并二氮杂衍生物，含有它们的组合物及其在治疗中的用途
公开(公告)号：US5597915A
公开(公告)日：1997-01-28
申请号：US295918
申请日：1994-09-15
申请人： Mark S. Chambers , Stephen R. Fletcher , Victor G. Matassa , Mark G. Bock
发明人： Mark S. Chambers , Stephen R. Fletcher , Victor G. Matassa , Mark G. Bock
IPC分类号： A61K31/55 , A61P3/08 , A61P9/00 , A61P25/04 , A61P25/24 , A61P25/26 , A61P25/28 , A61P43/00 , C07D413/12 , C07D417/12 , C07D403/12
CPC分类号： C07D413/10
摘要： Compounds of Formula (I), and salts and prodrugs thereof wherein: R.sup.1 is H, certain optionally substituted C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 represents a group (a) wherein X is O, S or NR.sup.8 where R.sup.8 is H or C.sub.1-4 alkyl; one of Z and Y is C.dbd.O and the other is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-4 alkyl; R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; R.sup.4 is C.sub.3-10 cycloalkyl; n is 0, 1, 2 or 3, and are CCK and/or gastrin antagonists, which compounds and compositions thereof are useful in therapy.
摘要翻译： PCT No.PCT / GB93 / 00535 Sec。 371日期1994年9月15日 102（e）1994年9月15日PCT 1993年3月15日PCT公布。公开号WO93 / 19063 （I）化合物及其盐和前体药物其中：R 1是H，某些任选取代的C 1-6烷基或C 3-7环烷基; R2表示其中X为O，S或NR8的基团（a），其中R8为H或C1-4烷基; Z和Y之一是C = O，另一个是O，S或NR 9，其中R 9是H或C 1-4烷基; R3是C1-6烷基，卤素或NR6R7; R4为C3-10环烷基; n为0,1,2或3，为CCK和/或胃泌素拮抗剂，其化合物及其组合物可用于治疗。

2. 发明授权

US5026851A Pyrido[2,3-]pyrimidine derivatives 失效
标题翻译：吡啶并[2,3]嘧啶衍生物
公开(公告)号：US5026851A
公开(公告)日：1991-06-25
申请号：US341497
申请日：1989-04-21
申请人： Edward C. Taylor , George P. Beardsley , Peter J. Harrington , Stephen R. Fletcher
发明人： Edward C. Taylor , George P. Beardsley , Peter J. Harrington , Stephen R. Fletcher
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , Y02P20/55
摘要： 2,4-Diamino- and 2-amino-4-hydroxy- derivatives of N-(4-[2-(pyrido[2,3-d]pyrimidin-6-yl)alkyl]benzoyl-)-L-glutamic acids, and the corresponding 5,6,7,8-tetrahydro compounds are antineoplastic agents.The compounds are prepared by hydrolytic or hydrogenolytic removal of carboxylic acid protecting groups from the correspondingly protected glutamic acid derivatives.A typical embodiment is N-(4-[2-(2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)ethyl]benzoyl)-L-glutamic acid.
摘要翻译： N-（4- [2-（吡啶并[2,3-d]嘧啶-6-基）烷基]苯甲酰基） - L-谷氨酸的2,4-二氨基 - 和2-氨基-4-羟基衍生物，相应的5,6,7,8-四氢化合物是抗肿瘤剂。通过水解或氢解除去相应保护的谷氨酸衍生物的羧酸保护基来制备化合物。典型的实施方案是N-（4- [2-（2-氨基-4-羟基-5,6,7,8-四氢吡啶并[2,3-d]嘧啶-6-基）乙基]苯甲酰基）谷氨酸。

3. 发明授权

US4684653A Pyrido(2,3-d)pyrimidine derivatives 失效
标题翻译：吡啶并（2,3-d）嘧啶衍生物
公开(公告)号：US4684653A
公开(公告)日：1987-08-04
申请号：US835457
申请日：1986-03-03
申请人： Edward C. Taylor , George P. Beardsley , Peter J. Harrington , Stephen R. Fletcher
发明人： Edward C. Taylor , George P. Beardsley , Peter J. Harrington , Stephen R. Fletcher
IPC分类号： C07D471/04 , A61K31/505 , C07D475/04 , C07D475/08
CPC分类号： C07D471/04 , Y02P20/55
摘要： 2,4-Diamino- and 2-amino-4-hydroxy- derivatives of N-(4-[1-(pyrido[2,3-d]pyrimidin-6-yl)alk-2-yl]-benzoyl)-L-glutamic acids, and the corresponding 5,6,7,8-tetrahydro compounds are antineoplastic agents.The compounds are prepared by hydrolytic or hydrogenolytic removal of carboxylic acid protecting groups from the correspondingly protected glutamic acid derivatives.A typical embodiment is N-(4-[2-(2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)ethyl]benzoyl)-L-glutamic acid.
摘要翻译： N-（4- [1-（吡啶并[2,3-d]嘧啶-6-基）烷-2-基] - 苯甲酰基） - 的2,4-二氨基 - 和2-氨基-4-羟基 - L-谷氨酸和相应的5,6,7,8-四氢化合物是抗肿瘤剂。通过水解或氢解除去相应保护的谷氨酸衍生物的羧酸保护基来制备化合物。典型的实施方案是N-（4- [2-（2-氨基-4-羟基-5,6,7,8-四氢吡啶并[2,3-d]嘧啶-6-基）乙基]苯甲酰基）谷氨酸。

4. 发明授权

US5332135A Apparatus for protecting watches and the like 失效
标题翻译：用于保护手表等的装置
公开(公告)号：US5332135A
公开(公告)日：1994-07-26
申请号：US981175
申请日：1992-11-24
申请人： Stephen R. Fletcher
发明人： Stephen R. Fletcher
IPC分类号： G04B37/00
CPC分类号： G04B37/005
摘要： The present invention provides an apparatus for protecting an instrument, such as a wrist-mounted time keeping instrument, from damage or loss. Lengths of flexible material are used for shielding the attaching band of the instrument from the surrounding environment. The flexible material is formed into a band to encircle the user's limb using a hook and loop fastener. A channel is formed on the underside of the flexible material to hold the attaching band in place and to seal out containments found in the surrounding environment. The apparatus is used without removing or modifying the existing attaching band of the instrument. A cover hides the instrument and also seals the instrument from the surrounding environment. The cover is a stretchable cover which has an open position allowing easy access to the instrument and a closed position which seals the instrument from the surrounding environment. The apparatus provides the advantage of being lockable to the attaching band and the instrument preventing loss and damage but yet is removable therefrom without removing the instrument from the limb of the user. The apparatus has applications with many different types of instruments and in many different applications such as sporting activities and work activities.
摘要翻译：本发明提供一种用于保护诸如手腕安装的时间保持仪器的仪器免受损坏或损失的装置。柔性材料的长度用于屏蔽仪器的附着带与周围环境。柔性材料被形成为使用钩环紧固件包围使用者肢体的带。在柔性材料的下侧上形成通道以将附接带固定就位并密封在周围环境中发现的容纳物。使用该装置而不去除或修改仪器的现有附着带。盖子隐藏仪器，并将仪器与周围环境密封。盖子是可拉伸的盖子，其具有打开位置，允许容易地进入仪器，并且闭合位置将仪器与周围环境密封。该装置具有可锁定到附接带和仪器的优点，防止损失和损坏，但是可从其移除，而不用将仪器从使用者的肢体移除。该设备具有许多不同类型的仪器以及许多不同的应用，例如体育活动和工作活动。

5. 发明授权

US4927828A Diastereoisomeric tetrahydropyrido-(2,3,d) pyrimidine derivatives 失效
标题翻译：非对映异构体四氢吡啶并（2,3，d）嘧啶衍生物
公开(公告)号：US4927828A
公开(公告)日：1990-05-22
申请号：US220944
申请日：1988-06-28
申请人： Edward C. Taylor , George P. Beardsley , Chuan Shih , Stephen R. Fletcher
发明人： Edward C. Taylor , George P. Beardsley , Chuan Shih , Stephen R. Fletcher
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , Y02P20/55
摘要： The diastereoisomeric forms of N-(4-[2-(2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido[2,3-d]-pyrimidin-6-yl)ethyl]benzoyl)-L-glutamic acid are antineoplastic agents.The compounds are prepared by separation of the diastereoisomeric form of the correspondingly protected glutamic derivatives and hydrolytic or hydrogenolytic removal of carboxylic acid and/or amino protecting groups.Typical embodiments are the (R,S) and (S,S) forms of N-(4-[2-(2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)ethyl]benzoyl)-L-glutamic acid.
摘要翻译： N-（4- [2-（2-氨基-4-羟基-5,6,7,8-四氢吡啶并[2,3-d]嘧啶-6-基）乙基]苯甲酰基）-L-非对映异构体形式谷氨酸是抗肿瘤药。通过分离相应保护的谷氨酸衍生物的非对映异构体形式和水解或解氢去除羧酸和/或氨基保护基来制备化合物。典型的实施方案是N-（4- [2-（2-氨基-4-羟基-5,6,7,8-四氢吡啶并[2,3-d]）的（R，S）和（S，S）嘧啶-6-基）乙基]苯甲酰基）-L-谷氨酸。

6. 发明授权

US4845216A Pyrido [2,3,d]pyrimidine derivatives 失效
标题翻译：吡啶并[2,3，d]嘧啶衍生物
公开(公告)号：US4845216A
公开(公告)日：1989-07-04
申请号：US74623
申请日：1987-07-17
申请人： Edward C. Taylor , George P. Beardsley , Peter J. Harrington , Stephen R. Fletcher
发明人： Edward C. Taylor , George P. Beardsley , Peter J. Harrington , Stephen R. Fletcher
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , Y02P20/55
摘要： 2,4-Diamino- and 2-amino-4-hydroxy- derivatives of N-(4-[2-(pyrido[2,3-d]pyrimidin-6-yl)alkyl]benzoyl)-L-glutamic acids, and the corresponding 5,6,7,8-tetrahydro compounds are antineoplastic agents. The compounds are prepared by hydrolytic or hydrogenolytic removal of carboxylic acid protecting groups from the correspondingly protected glutamic acid derivatives. A typical embodiment is N-)4-[2-(2-amino-4-hydroxy-5,6,7,8-tetrahydropyrido[2,3-d]pyrimidin-6-yl)ethyl]benzoyl)-L-glutamic acid.
摘要翻译： N-（4- [2-（吡啶并[2,3-d]嘧啶-6-基）烷基]苯甲酰基）-L-谷氨酸的2,4-二氨基 - 和2-氨基-4-羟基 - 相应的5,6,7,8-四氢化合物是抗肿瘤剂。通过水解或氢解除去相应保护的谷氨酸衍生物的羧酸保护基来制备化合物。典型的实施方案是N-）4- [2-（2-氨基-4-羟基-5,6,7,8-四氢吡啶并[2,3-d]嘧啶-6-基）乙基]苯甲酰基）谷氨酸。

7. 发明授权

US4516529A Aquarium 失效
标题翻译：水族馆
公开(公告)号：US4516529A
公开(公告)日：1985-05-14
申请号：US409528
申请日：1982-08-19
申请人： Vincent Lotito , Stephen R. Fletcher
发明人： Vincent Lotito , Stephen R. Fletcher
IPC分类号： A01K63/00
CPC分类号： A01K63/003
摘要： An aquarium for housing fish and other aquatic life if formed within a pyramidal housing. The upper portion of the housing is formed of transparent triangular walls which enclose the water for the fish while permitting viewing of the fish. The lower portion of the housing serves as a base for supporting the water, and includes a drawer which holds filtration, heating and aeration equipment while permitting ready access for servicing of the equipment. Lighting is provided by an internal pyramidal light situated at the apex of the housing within the walls, the location permitting lighting of the entire water surface without any significant heating of the walls. All plumbing connections for treatment of the water are made through the floor of the chamber holding the water, thereby avoiding the presence of unsightly hoses and tubing. By the placing of the filtering equipment below the water chamber, the filtering system is able to self-prime, thereby eliminating the process of siphoning in the caring of the aquarium.
摘要翻译：如果在一个金字塔形的房屋内形成，就可以容纳鱼类和其他水生生物的水族馆。壳体的上部由透明的三角形壁构成，其围绕鱼的水，同时允许观察鱼。壳体的下部用作支撑水的基座，并且包括保持过滤，加热和曝气设备的抽屉，同时允许便于维修设备。照明由位于墙壁内的壳体顶点处的内部锥形光提供，允许整个水面照明的位置，而不会对壁进行任何显着的加热。用于处理水的所有管道连接通过容纳水的室的地板进行，从而避免存在难看的软管和管道。通过将过滤设备放置在水室下方，过滤系统能够自给自足，从而消除了虹吸在水族箱中的过程。

8. 发明授权

US5618812A Benzodiazepine derivatives 失效
标题翻译：苯并二氮杂衍生物
公开(公告)号：US5618812A
公开(公告)日：1997-04-08
申请号：US374748
申请日：1995-01-26
申请人： Jose L. Castro Pineiro , William R. Carling , Mark S. Chambers , Stephen R. Fletcher , Sarah C. Hobbs , Victor G. Matassa , Kevin W. Moore , Graham A. Showell , Michael G. Russell
发明人： Jose L. Castro Pineiro , William R. Carling , Mark S. Chambers , Stephen R. Fletcher , Sarah C. Hobbs , Victor G. Matassa , Kevin W. Moore , Graham A. Showell , Michael G. Russell
IPC分类号： A61K31/55 , A61K31/551 , A61K31/5513 , A61P1/00 , A61P1/04 , A61P1/12 , A61P25/00 , A61P25/04 , A61P25/16 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/26 , A61P25/30 , A61P27/06 , A61P35/00 , A61P39/00 , A61P43/00 , C07D221/24 , C07D243/14 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D413/04 , C07D453/06 , C07D471/08 , C07D487/08 , C07D491/10 , C07D491/107 , C07D491/113
CPC分类号： C07D401/04 , C07D221/24 , C07D243/14 , C07D401/12 , C07D403/04 , C07D453/06 , C07D487/08 , C07D491/10
摘要： Compounds of Formula (I), and salts and prodrugs thereof, wherein R.sup.1 represents H, optionally substituted C.sub.1-6 alkyl or C.sub.3-7 cycloalkyl; R.sup.2 is NHR.sup.12 or (CH.sub.2).sub.s R.sup.13 where 5 is 0, 1 or 2; R.sup.3 represents C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; R.sup.4 and R.sup.5 are H, C.sub.1-12 alkyl optionally substituted by NR.sup.9 R.sup.9' or an azacyclic or azabicyclic group, optionally substituted C.sub.4-9 cycloalkyl, C.sub.4-9 cycloalkyl C.sub.1-4 alkyl, aryl, arylC.sub.1-6 alkyl or azacyclic or azabicyclic groups, or R.sup.4 and R.sup.5 together form the residue of an optionally substituted azacyclic or azabicyclic ring system; x is 0, 1, 2 or 3; R.sup.12 is optionally substituted phenyl or pyridyl; R.sup.13 represents a group (A) wherein R.sup.14 is H or C.sub.1-6 alkyl; R.sup.15 is H, C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ; and the dotted line is an optional covalent bond; are CCK and/or gastrin antagonists useful in therapy. ##STR1##
摘要翻译： PCT No.PCT / GB93 / 01599 Sec。 371日期1995年1月26日 102（e）日期1995年1月26日PCT提交1993年7月28日PCT公布。出版物WO94 / 03437 日期：1994年2月17日式（I）化合物及其盐和前药，其中R 1表示H，任选取代的C 1-6烷基或C 3-7环烷基; R2是NHR12或（CH2）sR13，其中5是0,1或2; R 3表示C 1-6烷基，卤代或NR 6 R 7; R 4和R 5是H，任选地被NR 9 R 9'或氮杂环或氮杂双环基团任选取代的C 1-12烷基，任选取代的C 4-9环烷基，C 4-9环烷基C 1-4烷基，芳基，芳基C 1-6烷基或氮杂环或氮杂双环基，或R 4和R 5一起形成任选取代的氮杂环或氮杂双环系的残基; x为0,1,2或3; R 12是任选取代的苯基或吡啶基; R 13表示其中R 14为H或C 1-6烷基的基团（A） R 15是H，C 1-6烷基，卤素或NR 6 R 7; 并且虚线是任选的共价键; 是用于治疗的CCK和/或胃泌素拮抗剂。（图）（一）

9. 发明授权

US5451582A Benzodiazepine derivatives, compositions containing them and their use in therapy 失效
标题翻译：苯并二氮杂衍生物，含有它们的组合物及其在治疗中的用途
公开(公告)号：US5451582A
公开(公告)日：1995-09-19
申请号：US16646
申请日：1993-02-12
申请人： Mark S. Chambers , Victor G. Matassa , Stephen R. Fletcher
发明人： Mark S. Chambers , Victor G. Matassa , Stephen R. Fletcher
IPC分类号： C07D243/14 , C07D403/12 , C07D243/24 , A61K31/55
CPC分类号： C07D403/12 , C07D243/14
摘要： Compounds of formula (I), and salts and prodrugs thereof ##STR1## wherein: R.sup.1 is H, certain optionally substituted C.sub.1.6 alkyl, or C.sub.3-7 cycloalkyl;R.sup.2 is (CH.sub.2).sub.q -tetrazolyl optionally substituted in the tetrazole ring by C.sub.1-4 alkyl, (CH.sub.2).sub.q -imidazolyl (where q is 0, 1, 2 or 3), CONHSO.sub.2 R.sup.9, SO.sub.2 NHCOR.sup.9 (where R.sup.9 is C.sub.1-6 alkyl, optionally substituted aryl or trifluoromethyl). SO.sub.2 NHR.sup.10 (where R.sup.10 is a nitrogen containing heterocycle), cyclopropyl or (CH.sub.2), CO.sub.2 H, where n is 1 or 2;R.sup.3 is C.sub.1-6 alkyl, halo or NR.sup.6 R.sup.7 ;R.sup.4 is C.sub.1-7 straight or branched chain alkyl; andx is 0, 1, 2 or 3;are CCK and/or gastrin receptor antagonists. They and compositions thereof are useful in therapy.
摘要翻译：式（I）化合物及其盐和前药其中：R 1为H，某些任选取代的C 1-6烷基或C 3-7环烷基; （CH 2）q-咪唑基（其中q为0,1,2或3），CONHSO 2 R 9，SO 2 NHCOR 9（其中R 9为C 1-6烷基，任选地为（CH 2）q-四唑基）取代的芳基或三氟甲基）。 SO2NHR10（其中R10是含氮杂环），环丙基或（CH2），CO2H，其中n为1或2; R3是C1-6烷基，卤素或NR6R7; R4是C1-7直链或支链烷基; x为0,1,2或3; 是CCK和/或胃泌素受体拮抗剂。它们及其组合物可用于治疗。

10. 发明授权

US5556969A Benzodiazepine derivatives 失效
标题翻译：苯并二氮杂衍生物
公开(公告)号：US5556969A
公开(公告)日：1996-09-17
申请号：US496840
申请日：1995-06-29
申请人： Mark S. Chambers , Stephen R. Fletcher
发明人： Mark S. Chambers , Stephen R. Fletcher
IPC分类号： C07D243/14 , C07D243/24 , A61K31/55 , C07D403/12 , C07D413/12
CPC分类号： C07D243/14
摘要： Compounds of the formula (I): ##STR1## wherein R.sub.1 is hydrogen or specified optionally substituted alkyl, R.sup.2 is specified optionally substituted phenyl or pyridyl, x is 0, 1, 2 or 3, R.sup.3 is a specified alkyl, halo or amino and R.sup.4 is specified cycoalkyl or bicycloalkyl; and salts and prodrugs thereof, are useful as antagonists of cholecystokin and gastrin receptors.
摘要翻译：式（I）的化合物：其中R 1是氢或指定的任选取代的烷基，R 2是任选取代的苯基或吡啶基，x是0,1,2或3，R3是指定的烷基，卤代或氨基，R4为特定的环烷基或双环烷基; 其盐和前药可用作胆囊收缩素和胃泌素受体的拮抗剂。

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