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1. 发明授权

US06479527B1 Bicyclic pyrrole derivatives as MCP-1 inhibitors 失效
标题翻译：双环吡咯衍生物作为MCP-1抑制剂
公开(公告)号：US06479527B1
公开(公告)日：2002-11-12
申请号：US09626378
申请日：2000-07-26
申请人： Andrew J. Barker , Alan W Faull , Jason G. Kettle
发明人： Andrew J. Barker , Alan W Faull , Jason G. Kettle
IPC分类号： A61K31407
CPC分类号： C07D487/04 , C07D491/04 , C07D495/04 , C07D513/04
摘要： A pharmaceutical composition comprising a compound of formula (I): or a pharmaceutically acceptable salt, ester or amide thereof, which is an inhibitor of monocyte chemoattractant protein-1 and wherein A and B together form an optionally substituted 5-member aromatic ring which includes at least one heteroatom; R1 is an optionally substituted aryl or heteroaryl ring; R2 is selected from a range of organic groups including carboxy, and R3 is hydrogen, or a range of organic groups; in combination with a pharmaceutically acceptable carrier. Certain compounds of formula (I) are novel and these form a further aspect of the invention.
摘要翻译：一种药物组合物，其包含式（I）化合物或其药学上可接受的盐，酯或酰胺，其为单核细胞趋化蛋白-1的抑制剂，其中A和B一起形成任选取代的5元芳环，其包括至少一个杂原子; R1是任选取代的芳基或杂芳基环; R2选自一系列有机基团，包括羧基，R3是氢或一定范围的有机基团; 与药学上可接受的载体组合。某些式（I）化合物是新的，这些是本发明的另一方面。

2. 发明授权

US5089499A Quinazoline derivatives possessing anti-tumor activity 失效
标题翻译：具有抗肿瘤活性的喹诺酮衍生物
公开(公告)号：US5089499A
公开(公告)日：1992-02-18
申请号：US450670
申请日：1989-12-14
申请人： Andrew J. Barker , Leslie R. Hughes , Peter R. Marsham , John Oldfield , Stephen J. Pegg
发明人： Andrew J. Barker , Leslie R. Hughes , Peter R. Marsham , John Oldfield , Stephen J. Pegg
IPC分类号： A61K31/505 , A61K31/517 , A61P35/00 , C07D20060101 , C07D239/90 , C07D239/95 , C07D239/96 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D401/12 , C07D239/90 , C07D239/95 , C07D239/96 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： The invention relates to quinazoline derivatives, or pharmaceutically-acceptable salts thereof, which possess anti-tumor activity; to processes for their manufacture; and to pharmaceutical compositions containing them. The invention provides a quinazoline of the formula: ##STR1## wherein R.sup.1 is hydrogen or amino, or alkyl or alkoxy each of up to 6 carbon atoms; or R.sup.1 is substituted alkyl or alkoxy each of up to 3 carbon atoms;R.sup.2 is hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, halogenoalkyl or cyanoalkyl each of up to 6 carbon atoms;Ar is phenylene or heterocyclene;L is a group of the formula --CO.NH--, --NH.CO--, --CO.NR.sup.3 --, --NR.sup.3. CO--, --CH.dbd.CH--, --CH.sub.2 O--, --OCH.sub.2, --CH.sub.2 S--, --SCH.sub.2 --, --CO.CH.sub.2 --, --CH.sub.2.CO-- or --CO.O--, wherein R.sup.3 is alkyl of up to 6 carbon atoms; andY is aryl or heteroaryl or a hydrogenated derivative thereof: orY is a group of the formula --A--Y.sup.1 in which A is alkylene, cycloalkylene, alkenylene or alkynylene each of up to 6 carbon atoms and Y.sup.1 is aryl or heteroaryl or a hydrogenated derivative thereof;or a pharmaceutically-acceptable salt thereof.

3. 发明授权

US4795748A Antibacterial 7-oxo-4-thia-1-azabicyclo[3,2,0]hept-2-ene derivatives 失效
标题翻译：抗菌7-氧代-4-硫杂-1-氮杂双环[3,2,0]庚-2-烯衍生物
公开(公告)号：US4795748A
公开(公告)日：1989-01-03
申请号：US749384
申请日：1985-06-27
申请人： Barry C. Ross , Michael D. Cooke , Nicholas I. Carruthers , Andrew J. Barker
发明人： Barry C. Ross , Michael D. Cooke , Nicholas I. Carruthers , Andrew J. Barker
IPC分类号： A61K31/397 , A61K31/425 , A61P31/04 , C07C69/90 , C07D205/08 , C07D205/09 , C07D499/88 , C07D499/897 , C07F7/18 , C07D499/00
CPC分类号： C07C69/90 , C07D205/08 , C07D205/09 , C07D499/88 , C07F7/186 , C07F7/1896
摘要： A compound of the formula I ##STR1## in which R.sup.1 represents a hydrogen atom or an alkyl group having from 1 to 4 carbon atoms, the --CONHR.sup.1 group being present at the 3- or 4-position on the phenyl ring, and esters thereof at the 2-carboxyl group and/or at the 8-hydroxy group, have antibacterial and/or .beta.-lactamase inhibiting activity.
摘要翻译：其中R 1表示氢原子或具有1至4个碳原子的烷基的式I化合物（I），-CONHR 1基团存在于苯环上的3-或4-位，及其在2-羧基和/或8-羟基的酯具有抑制和/或β-内酰胺酶抑制活性。

4. 发明授权

US06876441B2 Optical sensor for distance measurement 失效
标题翻译：用于距离测量的光学传感器
公开(公告)号：US06876441B2
公开(公告)日：2005-04-05
申请号：US10156126
申请日：2002-05-29
申请人： Andrew J. Barker
发明人： Andrew J. Barker
IPC分类号： G01C3/06 , G01S7/481 , G01S7/491 , G01S7/493 , G01S17/36 , G01C3/08
CPC分类号： G01S7/4812 , G01S7/4915 , G01S7/493 , G01S17/36
摘要： Apparatus and method are provided for distance measurement to a remote surface using high frequency modulated transmitted and reflected laser beams and phase-shift calculations. To improve phase-shift resolution, the reflected bean is further modulated, before detection, at a high frequency similar yet different from that of the transmitted beam so as create a resulting detector signal having at least a lower frequency signal which is easily detected by a response limited detector. The lower frequency signal retains the phase-shift information and thus enables determination of the phase-shift information with stable, inexpensive low-frequency optical detectors. Three-dimensional mapping can performed wherein one or more apparatus employ a plurality of detectors or a scanner producing a plurality of sequential reflected beams, each of which results in a plurality of phase-shift information for an area on the surface.
摘要翻译：提供了使用高频调制的发射和反射激光束和相移计算对远程表面的距离测量的装置和方法。为了提高相移分辨率，反射的豆在检测之前被进一步调制，其频率与发射波束的高频相似但不同，从而产生具有至少较低频率信号的结果检测器信号，该信号易于被响应限制检测器。低频信号保持相移信息，从而能够利用稳定，廉价的低频光检测器来确定相移信息。可以执行三维映射，其中一个或多个装置采用多个检测器或产生多个顺序反射光束的扫描器，每个反射光束导致表面上的区域的多个相移信息。

5. 发明授权

US5569658A Tricyclic derivatives 失效
标题翻译：三环衍生物
公开(公告)号：US5569658A
公开(公告)日：1996-10-29
申请号：US275754
申请日：1994-07-19
申请人： Andrew J. Barker
发明人： Andrew J. Barker
IPC分类号： A61K31/505 , A61P35/00 , A61P43/00 , C07D471/04 , C07D487/04 , C07D498/04 , C07D513/04 , C07D237/26 , A61K31/495 , C07D239/70
CPC分类号： C07D487/04
摘要： The invention concerns tricyclic derivatives of the formula I ##STR1## wherein R.sup.1 and R.sup.2 together form an optionally substituted group of the formula --N.dbd.CH--NH--, --N.dbd.CH--O--, --N.dbd.CH--S--, --N.dbd.N--NH--, --NH--N.dbd.CH--, --NH--CH.dbd.CH--. --NH--CO--NH--, --NH--CO--O--, --NH--CO--S--, --NH--NH--CO--, --N.dbd.CH--CH.dbd.N--, --N.dbd.N--CH.dbd.CH--, --N.dbd.CH--N.dbd.CH--, --N.dbd.CH--CH.dbd.N--, --NH--CO--CH.dbd.CH-- or --N.dbd.CH--CO--NH--; m is 1, 2 or 3 and R.sup.3 includes hydrogen, halogeno and (1-4C)alkyl; or a pharmaceutically-acceptable salt thereof;processes for their preparation; pharmaceutical compositions containing them; and the use of the receptor tyrosine kinase inhibitory properties of the compounds. in the treatment of cancer.
摘要翻译：本发明涉及式I的三环衍生物，其中R 1和R 2一起形成式-N = CH-NH-，-N = CH-O-，-N = CH-S-， -N = N-NH-，-NH-N = CH-，-NH-CH = CH-。 -NH-CO-NH-，-NH-CO-O-，-NH-CO-S-，-NH-NH-CO-，-N = CH-CH = N-，-N = N-CH = CH - ，-N = CH-N = CH-，-N = CH-CH = N-，-NH-CO-CH = CH-或-N = CH-CO-NH-; m是1,2或3，R 3包括氢，卤素和（1-4C）烷基; 或其药学上可接受的盐; 其准备过程; 含有它们的药物组合物; 并使用受体酪氨酸激酶抑制化合物的性质。在治疗癌症。

6. 发明授权

US5457105A Quinazoline derivatives useful for treatment of neoplastic disease 失效
标题翻译：喹唑啉衍生物可用于治疗肿瘤性疾病
公开(公告)号：US5457105A
公开(公告)日：1995-10-10
申请号：US284293
申请日：1994-08-02
申请人： Andrew J. Barker
发明人： Andrew J. Barker
IPC分类号： A61K31/505 , A61K31/517 , A61P35/00 , C07D239/00 , C07D239/94 , C07D317/00 , C07D319/00 , C07D403/04 , C07D403/12 , C07D491/04 , C07D491/056 , A61K31/51 , A61K31/535 , C07D239/74 , C07D239/82
CPC分类号： C07D403/04 , C07D239/94 , C07D491/04
摘要： The invention concerns quinazoline derivatives of the formula I ##STR1## wherein m is 1, 2 or 3 and each R.sup.1 includes hydroxy, amino, carboxy, carbamoyl, ureido, (1-4C)alkoxycarbonyl, N-(1-4C)alkylcarbamoyl, N,N-di-[(1-4C)alkyl]carbamoyl, hydroxyamino, (1-4C)alkoxyamino, (2-4C)alkanoyloxyamino, trifluoromethoxy, (1-4C)alkyl, (1-4C)alkoxy and (1-3C)alkylenedioxy;n is 1 or 2 and each R.sup.2 includes hydrogen, hydroxy, halogeno, trifluoromethyl, amino, nitro, cyano and (1-4C)alkyl;or a pharmaceutically-acceptable salt thereof;processes for their preparation; pharmaceutical compositions containing them; and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of cancer.
摘要翻译：本发明涉及式I的喹唑啉衍生物，其中m为1,2或3，并且每个R 1包括羟基，氨基，羧基，氨基甲酰基，脲基，（1-4C）烷氧基羰基，N-（1-4C）烷基氨基甲酰基 N，N-二 - [（1-4C）烷基]氨基甲酰基，羟基氨基，（1-4C）烷氧基氨基，（2-4C）烷酰氧基氨基，三氟甲氧基，（1-4C）烷基，（1-4C）烷氧基和（ 1-3C）亚烷基二氧基; n为1或2，每个R2包括氢，羟基，卤代，三氟甲基，氨基，硝基，氰基和（1-4C）烷基; 或其药学上可接受的盐; 其准备过程; 含有它们的药物组合物; 以及使用受体酪氨酸激酶抑制化合物治疗癌症的性质。

7. 发明授权

US5280027A Anti-tumor compounds 失效
标题翻译：抗肿瘤化合物
公开(公告)号：US5280027A
公开(公告)日：1994-01-18
申请号：US708046
申请日：1991-05-30
申请人： Robert G. Andrew , Andrew J. Barker , Francis T. Boyle , James M. Wardleworth
发明人： Robert G. Andrew , Andrew J. Barker , Francis T. Boyle , James M. Wardleworth
IPC分类号： A61K31/505 , A61K31/517 , A61P35/00 , C07D239/88 , C07D239/90 , C07D239/95 , C07D239/96 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号： C07D403/12 , C07D239/90 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The invention relates to quinazoline derivatives, or pharmaceutically-acceptable salts thereof, which possess anti-tumour activity; to processes for their manufacture; and to pharmaceutical compositions containing them.The invention provides a quinazoline of the formula: ##STR1## wherein R.sup.1 includes hydrogen, amino and alkyl or alkoxy each of up to 4 carbon atoms;R.sup.2 includes hydrogen, alkyl, hydroxyalkyl and halogenoalkyl each of up to 4 carbon atoms;R.sup.3 is hydrogen or alkyl or up to 3 carbon atoms;Ar is phenylene or heterocyclene;L is a group of the formula --CO.NH--, --NH.CO--, --CO.NR.sup.4 --, --NR.sup.4.CO--, --CH.dbd.CH-- or --CO.O--, wherein R.sup.4 is alkyl of up to 4 carbon atoms; and Y is a branched alkyl group bearing substituents Y.sup.2 and Y.sup.3 the definition of each independently including hydroxy, cyano, aryl and heteroaryl, and the definition of Y.sup.3 also optionally including sulpho, N-phenylsulphonylcarbamoyl and 5-tetrazolyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译：本发明涉及具有抗肿瘤活性的喹唑啉衍生物或其药学上可接受的盐; 制造过程; 以及含有它们的药物组合物。本发明提供下式的喹唑啉：（*化学结构*）其中R1包括氢，氨基和至多4个碳原子的烷基或烷氧基; R2包括至多4个碳原子的氢，烷基，羟基烷基和卤代烷基; R3是氢或烷基或至多3个碳原子; Ar是亚苯基或杂环烯; L是式-CO.NH-，-NH.CO-，-CO.NR4-，-NR4CO-，-CH = CH-或-CO.O-的基团，其中R4是直至 4个碳原子; Y是带有取代基Y2和Y3的支链烷基，其各自独立地包括羟基，氰基，芳基和杂芳基，Y 3的定义也任选地包括磺基，N-苯基磺酰基氨基甲酰基和5-四唑基; 或其药学上可接受的盐。

8. 发明授权

US4455086A Optical test apparatus for examining an object 失效
标题翻译：用于检查物体的光学测试装置
公开(公告)号：US4455086A
公开(公告)日：1984-06-19
申请号：US347132
申请日：1982-02-09
申请人： Robert N. West , Andrew J. Barker
发明人： Robert N. West , Andrew J. Barker
IPC分类号： G01N21/89 , G01N21/00
CPC分类号： G01N21/8901
摘要： Test apparatus and method for testing for faults in, for example, transparent sheet material in which two parallel beams of light separated by a distance "w" are passed through a grating having, for example, light transmitting and absorbing areas separated by a distance "w", so that as the two beams are scanned across the object and the grating the light output through the grating is generally constant. If, however, there are faults which displace one beam with respect to the other, then the spacing between the beams will change so the light output will vary from the norm. Furthermore, if there is a fault which would cause attenuation of the two beams, then the light output will again vary from the norm.
摘要翻译：用于测试例如透明片材的测试装置和方法，其中将两个平行光束分开一段距离“w”的光束通过光栅，该光栅具有例如隔开距离“ w“，使得当两个光束跨过物体和光栅扫描时，通过光栅输出的光通常是恒定的。然而，如果存在相对于另一个移动一个光束的故障，则光束之间的间隔将改变，使得光输出将随规范变化。此外，如果存在将导致两个光束衰减的故障，则光输出将再次从标准变化。

9. 发明授权

US06513136B1 Communications receiver arrangement 有权
标题翻译：通信接收机布置
公开(公告)号：US06513136B1
公开(公告)日：2003-01-28
申请号：US09432317
申请日：1999-11-02
申请人： Andrew J. Barker
发明人： Andrew J. Barker
IPC分类号： G06F1100
CPC分类号： H04L25/063 , H04L1/0045 , H04L1/0057
摘要： A receiver in a digital communications system, in which the digital data occupy a number of levels, equalises the erroneous-count rates for the various data levels by deriving the count rates for the levels, comparing these count rates with each other and using the comparison result to adjust the threshold level which is used to detect the received data train. The error-counts are preferably derived as a byproduct of a Forward Error Correction system already available for performing normal error correction on the received data. The receiver arrangement is envisaged to find predominant application in a two-level system involving logical “1”'s and “0”'s, though it is applicable also to systems with three or more levels.
摘要翻译：在数字通信系统中的数字数据占用多个级别的接收机，通过导出电平的计数率，将这些计数率相互比较并使用比较来均衡各种数据电平的错误计数率结果调整用于检测接收到的数据序列的阈值水平。错误计数优选地被导出为已经可用于对所接收的数据执行正常纠错的前向纠错系统的副产品。接收机布置被设想在涉及逻辑“1”和“0”的两级系统中找到主要应用，尽管它也适用于具有三个或更多个级别的系统。

10. 发明授权

US5616582A Quinazoline derivatives as anti-proliferative agents 失效
标题翻译：喹唑啉衍生物作为抗增殖剂
公开(公告)号：US5616582A
公开(公告)日：1997-04-01
申请号：US490666
申请日：1995-06-15
申请人： Andrew J. Barker
发明人： Andrew J. Barker
IPC分类号： A61K31/505 , A61K31/517 , A61P35/00 , C07D239/00 , C07D239/94 , C07D317/00 , C07D319/00 , C07D403/04 , C07D403/12 , C07D491/04 , C07D491/056 , C07D403/00 , A61K31/51 , A61K31/535 , C07D239/82
CPC分类号： C07D403/04 , C07D239/94 , C07D491/04
摘要： The invention concerns quinazoline derivatives of the formula I ##STR1## wherein m is 1, 2 or 3 and each R.sup.1 includes hydroxy, amino, carboxy, carbamoyl, ureido, (1-4C)alkoxycarbonyl, N-(1-4C)alkylcarbamoyl, N,N-di-[(1-4C)alkyl]carbamoyl, hydroxyamino, (1-4C)alkoxyamino, (2-4C)alkanoyloxyamino, trifluoromethoxy, (1-4C)alkyl, (1-4C)alkoxy and (1-3C)alkylenedioxy;n is 1 or 2 and each R.sup.2 includes hydrogen, hydroxy, halogeno, trifluoromethyl, amino, nitro, cyano and (1-4C)alkyl; or a pharmaceutically-acceptable salt thereof;processes for their preparation; pharmaceutical compositions containing them; and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of cancer.
摘要翻译：本发明涉及式I的喹唑啉衍生物，其中m为1,2或3，并且每个R 1包括羟基，氨基，羧基，氨基甲酰基，脲基，（1-4C）烷氧基羰基，N-（1-4C）烷基氨基甲酰基 N，N-二 - [（1-4C）烷基]氨基甲酰基，羟基氨基，（1-4C）烷氧基氨基，（2-4C）烷酰氧基氨基，三氟甲氧基，（1-4C）烷基，（1-4C）烷氧基和（ 1-3C）亚烷基二氧基; n为1或2，每个R2包括氢，羟基，卤代，三氟甲基，氨基，硝基，氰基和（1-4C）烷基; 或其药学上可接受的盐; 其准备过程; 含有它们的药物组合物; 以及使用受体酪氨酸激酶抑制化合物治疗癌症的性质。

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