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1. 发明授权

US5608070A Enantioselective process for the preparation of chiral triaryl derivatives and chiral intermediates for use therein 失效
标题翻译：用于制备手性三芳基衍生物和手性中间体的对映选择性方法
公开(公告)号：US5608070A
公开(公告)日：1997-03-04
申请号：US361439
申请日：1994-12-21
申请人： Rikki P. Alexander , Graham J. Warrellow , John C. Head , Ewan C. Boyd , John R. Porter
发明人： Rikki P. Alexander , Graham J. Warrellow , John C. Head , Ewan C. Boyd , John R. Porter
IPC分类号： C07D233/64 , C07D213/30 , C07D213/32 , C07D213/55 , C07D213/56 , C07D401/06 , C07D409/06 , C07D417/06 , C07D417/14 , C07D417/00
CPC分类号： C07D213/30 , C07D417/06 , C07D417/14
摘要： An enantioselective multi-stage process is described which uses as a starting material an .alpha.,.beta.-unsaturated olefin of formula (1):Ar--CH.dbd.C(R.sup.4)COAux (1)where Ar and R.sup.4, which may be the same or different, is each a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; and Aux is the residue of a chiral (R- or S-) auxiliary.In the process, the olefin is converted to a chiral triarylethane which is of use in medicine.
摘要翻译：描述了使用式（1）的α，β-不饱和烯烃作为原料的对映选择性多阶段方法：Ar-CH = C（R 4）COAux（1）其中Ar和R 4可以相同或各自是任选含有一个或多个选自氧，硫或氮原子的杂原子的单环或双环芳基; Aux是手性（R-或S-）辅助物的残基。在此过程中，烯烃被转化为在医学上有用的手性三芳基乙烷。

2. 发明授权

US5622977A Tri-substituted (aryl or heteroaryl) derivatives and pharmaceutical compositions containing the same 失效
标题翻译：三取代（芳基或杂芳基）衍生物和含有它们的药物组合物
公开(公告)号：US5622977A
公开(公告)日：1997-04-22
申请号：US474214
申请日：1995-06-07
申请人： Graham J. Warrellow , Ewan C. Boyd , Rikki P. Alexander , John C. Head
发明人： Graham J. Warrellow , Ewan C. Boyd , Rikki P. Alexander , John C. Head
IPC分类号： C07C43/235 , C07C59/72 , A61K31/44 , C07D213/04 , C07D405/10 , C07D409/10
CPC分类号： C07C43/235 , C07C59/72
摘要： Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is a substituted or unsubstituted alkyl; X is --O--, --S-- or --N(R.sup.8)--, where R.sup.8 is hydrogen or alkyl; R.sup.2 is substituted or unsubstituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or substituted or unsubstituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 and R.sup.5, which may be the same or different, are each --(CH.sub.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group or monocyclic or bicyclic heteroaryl and n is integer of 0 to 3; R.sup.6 is hydrogen or substituted or unsubstituted alkyl; R.sup.7 is hydrogen or substituted or unsubstituted alkyl; and the salts, solvates, hydrates and N-oxides thereof. Compounds according to the invention are potent, selective and orally active PDE IV inhibitors and are useful in the prophylaxis and treatment of asthma and other diseases.
摘要翻译：其中Y为卤素或-OR 1，其中R 1为取代或未取代的烷基; X是-O - ， - S-或-N（R 8） - ，其中R 8是氢或烷基; R2是取代或未取代的烷基，烯基，环烷基或环烯基; R3是氢，卤素或-OR9，其中R9是氢或取代或未取代的烷基，烯基，烷氧基烷基或烷酰基，或甲酰基，甲酰氨基或硫代羧酰胺基; R 4和R 5可以相同或不同，各自为 - （CH 2）n Ar，其中Ar为单环或双环芳基或单环或双环杂芳基，n为0至3的整数; R6是氢或取代或未取代的烷基; R7是氢或取代或未取代的烷基; 及其盐，溶剂合物，水合物和N-氧化物。根据本发明的化合物是有效的，选择性和口服活性的PDE IV抑制剂，并且可用于预防和治疗哮喘和其它疾病。

3. 发明授权

US5580888A Styryl derivatives as anti-inflammatory agents 失效
标题翻译：苯乙烯基衍生物作为抗炎剂
公开(公告)号：US5580888A
公开(公告)日：1996-12-03
申请号：US462118
申请日：1995-06-05
申请人： Graham J. Warrellow , Ewan C. Boyd , Rikki P. Alexander
发明人： Graham J. Warrellow , Ewan C. Boyd , Rikki P. Alexander
IPC分类号： A61K31/085 , A61K31/09 , A61K31/10 , A61K31/135 , A61K31/415 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/443 , A61K31/4433 , A61P11/16 , A61P29/00 , A61P43/00 , C07C41/30 , C07C43/20 , C07C43/243 , C07C43/247 , C07C43/253 , C07C65/26 , C07C69/94 , C07D213/30 , C07D213/36 , C07D213/38 , C07D213/40 , C07D213/60 , C07D233/64 , C07D237/08 , C07D239/26 , C07D241/12 , C07D405/06 , C07D409/06 , C07D413/06 , C07D401/10 , C07D405/10 , C07D409/10
CPC分类号： C07D213/30 , C07C43/243 , C07C43/247 , C07C43/253 , C07C65/26 , C07C69/94 , C07D213/36 , C07D213/38 , C07D213/40 , C07D237/08 , C07D239/26 , C07D241/12 , C07D405/06
摘要： Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR.sup.1, wherein R.sup.1 is an optionally substituted alkyl group; X is --O--, --S-- or --N(R.sup.6)--, where R.sup.6 is a hydrogen atom or an alkyl group; R.sup.2 is an optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group; R.sup.3 and R.sup.4, which may be the same or different, is each a group --(CH.sup.2).sub.n Ar, where Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms and n is zero or an integer 1, 2 or 3; R.sup.5 is a hydrogen atom or an optionally substituted alkyl group; and the salts, solvates, hydrates and N-oxides. Compounds according to the invention are potent, selective and orally active PDE IV inhibitors and are useful in the prophylaxis and treatment of asthma.
摘要翻译：描述通式（1）的化合物其中Y是卤素原子或-OR1基团，其中R1是任意取代的烷基; X是-O - ， - S-或-N（R6） - ，其中R6是氢原子或烷基; R2是任选取代的烷基，烯基，环烷基或环烯基; R 3和R 4可以相同或不同，各自为 - （CH 2）nAr基团，其中Ar为任选含有一个或多个选自氧，硫或氮原子的杂原子的单环或双环芳基，n为零或整数1,2或3; R5是氢原子或任意取代的烷基; 和盐，溶剂合物，水合物和N-氧化物。根据本发明的化合物是有效的，选择性和口服活性的PDE IV抑制剂，并且可用于预防和治疗哮喘。

4. 发明授权

US5491147A Tri-substituted phenyl derivatives and their use in pharmaceutical compositions and methods of treatment 失效
标题翻译：三取代苯基衍生物及其在药物组合物和治疗方法中的应用
公开(公告)号：US5491147A
公开(公告)日：1996-02-13
申请号：US387551
申请日：1995-02-13
申请人： Ewan C. Boyd , Michael A. W. Eaton , Graham J. Warrellow
发明人： Ewan C. Boyd , Michael A. W. Eaton , Graham J. Warrellow
IPC分类号： C12N9/99 , A61K31/10 , A61K31/135 , A61K31/425 , A61K31/426 , A61K31/44 , A61K31/4409 , A61K31/4418 , A61K31/47 , A61K31/472 , A61K31/50 , A61K31/505 , A61P25/28 , A61P29/00 , A61P37/00 , A61P37/08 , A61P43/00 , C07C41/30 , C07C43/235 , C07C43/247 , C07C69/94 , C07C205/35 , C07C211/52 , C07C255/54 , C07C291/02 , C07C323/09 , C07C323/20 , C07D213/26 , C07D213/28 , C07D213/30 , C07D213/36 , C07D213/61 , C07D215/14 , C07D217/02 , C07D217/16 , C07D217/22 , C07D237/08 , C07D239/26 , C07D239/28 , C07D239/34 , C07D239/38 , C07D239/42 , C07D277/22 , C07D333/16 , C07F5/02
CPC分类号： C07D213/30 , C07C205/35 , C07C255/54 , C07C43/235 , C07C43/247 , C07C69/94 , C07D213/61 , C07D215/14 , C07D217/16 , C07D217/22 , C07D237/08 , C07D239/26 , C07D239/28 , C07D239/38 , C07D239/42 , C07D333/16 , C07C2101/08
摘要： Compounds of formula (1) ##STR1## are described wherein Y represents a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; R.sup.2 represents an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen or sulphur atoms or a group --N(R.sup.4)-- where R.sup.4 is a hydrogen atom or an alkyl group; X is --O--, --S--, or --N(R.sup.5)--, where R.sup.5 is a hydrogen or an alkyl group; with the proviso that when X is --O-- then R.sup.3 is not a 3-cyanamino-6-pyridazinyl or a 3-chloro-6-pyridazinyl group; and the salts, solvates, hydrates and N-oxides thereof.The compounds are selective and potent inhibitors of phosphodiesterase IV and are useful for the prophylaxis and treatment of inflammatory diseases and the alleviation of conditions associated with central nervous malfunction.
摘要翻译：其中Y表示卤素原子或-OR1基团，其中R1是任选取代的烷基;式（1）的化合物 R2表示任选取代的环烷基或环烯基; R3是任选地含有一个或多个选自氧或硫原子的杂原子的单环或双环芳基或基团-N（R 4） - ，其中R 4是氢原子或烷基; X是-O - ， - S-或-N（R 5） - ，其中R 5是氢或烷基; 条件是当X是-O-时，R 3不是3-氰氨基-6-哒嗪基或3-氯-6-哒嗪基; 及其盐，溶剂合物，水合物和N-氧化物。这些化合物是磷酸二酯酶IV的选择性和有效的抑制剂，并且可用于预防和治疗炎性疾病以及缓解与中枢神经功能障碍有关的病症。

5. 发明授权

US5633257A Cyclo(alkyl and alkenyl)phenyl-alkenylyl(aryl and heteroaryl)compounds and pharmaceutical compositions containing them 失效
标题翻译：环（烷基和烯基）苯基 - 烯基（芳基和杂芳基）化合物和含有它们的药物组合物
公开(公告)号：US5633257A
公开(公告)日：1997-05-27
申请号：US209419
申请日：1994-03-09
申请人： Graham J. Warrellow , Valerie A. Cole , Rikki P. Alexander
发明人： Graham J. Warrellow , Valerie A. Cole , Rikki P. Alexander
IPC分类号： A61K31/275 , A61K31/38 , A61K31/381 , A61K31/44 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4418 , A61K31/505 , A61P9/00 , A61P11/08 , A61P29/00 , A61P37/06 , A61P43/00 , C07C41/16 , C07C41/30 , C07C43/243 , C07C43/247 , C07C47/575 , C07C59/72 , C07C67/327 , C07C67/343 , C07C69/734 , C07C229/42 , C07C233/26 , C07C237/14 , C07C237/24 , C07C239/10 , C07C253/30 , C07C255/32 , C07C255/37 , C07C255/43 , C07C323/62 , C07C333/24 , C07D213/30 , C07D213/55 , C07D213/57 , C07D213/61 , C07D233/28 , C07D233/66 , C07D237/08 , C07D239/26 , C07D241/12 , C07D333/24 , C07D213/02
CPC分类号： C07D213/30 , C07C255/37 , C07C255/43 , C07D213/55 , C07D213/57 , C07D213/61 , C07D233/28 , C07D237/08 , C07D239/26 , C07D241/12 , C07D333/24 , C07C2101/08
摘要： Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR.sup.1, wherein R.sup.1 is an optionally substituted alkyl group; X is --O--, --S--, or --N(R.sup.6), wherein R.sup.6 is a hydrogen atom or an optionally substituted alkyl group; R.sup.2 is an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 and R.sup.4, which may be the same or different, is each a hydrogen atom or an optionally substituted alkyl, --CO.sub.2 R.sup.7 (wherein R.sup.7 is a hydrogen atom, am optionally substituted alkyl, aralkyl, aryl, aryloxyalkyl, alkanoyloxyalkyl or aroyloxyalkyl group), --CONR.sup.8 R.sup.9 (where R.sup.8 and R.sup.9, which may be the same or different, is as defined for R.sup.7), --CSNR.sup.8 R.sup.9, --CN or --CH.sub.2 CN group; Z is --(CH.sub.2).sub.n -- where n is zero or an integer 1, 2 or 3; R.sup.5 is an optionally substituted monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; and the salts, solvates, hydrates, prodrugs and N-oxides thereof. Compounds according to the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present.
摘要翻译：描述通式（1）的化合物其中Y是卤素原子或-OR1基团，其中R1是任意取代的烷基; X是-O - ， - S-或-N（R 6），其中R 6是氢原子或任选取代的烷基; R2是任选取代的环烷基或环烯基; R 3和R 4可以相同或不同，各自为氢原子或任选取代的烷基-CO 2 R 7（其中R 7为氢原子，任选取代的烷基，芳烷基，芳基，芳氧基烷基，烷酰氧基烷基或芳氧基烷基） -CONR 8 R 9（其中R 8和R 9可以相同或不同，如R7），-CSNR8R9，-CN或-CH2CN基团所定义; Z是 - （CH 2）n - ，其中n是0或整数1,2或3; R5是任选地含有一个或多个选自氧，硫或氮原子的杂原子的任选取代的单环或双环芳基; 及其盐，溶剂化物，水合物，前药和N-氧化物。根据本发明的化合物是有效和选择性的磷酸二酯酶IV型抑制剂，并且可用于预防和治疗诸如哮喘的疾病，其中存在不想要的炎症反应或肌肉痉挛。

6. 发明授权

US5177078A Piperazine derivatives 失效
标题翻译：哌嗪衍生物
公开(公告)号：US5177078A
公开(公告)日：1993-01-05
申请号：US768147
申请日：1991-09-30
申请人： Terence J. Ward , Graham J. Warrellow
发明人： Terence J. Ward , Graham J. Warrellow
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/4245 , A61K31/44 , A61K31/495 , A61K31/496 , A61K31/505 , A61P9/12 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P43/00 , C07D233/54 , C07D233/61 , C07D235/06 , C07D235/08 , C07D239/26 , C07D271/06 , C07D295/084 , C07D295/12 , C07D295/125 , C07D521/00
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D235/06 , C07D249/08 , C07D271/06 , C07D295/092 , C07D295/125
摘要： Compounds of formula ##STR1## where A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups,R is hydrogen or lower alkyl,R.sup.1 is an aryl or heteroaryl radical,R.sup.2 is a mono- or bicyclic heterocyclic radical,R.sup.3 is hydrogen, lower alkyl or hydroxy andR.sup.4 is a aryl or heteroaryl radical,and their pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents which may be used, for example, for the treatment of CNS--disorders such as anxiety.

7. 发明授权

US5169845A Piperazine derivatives 失效
标题翻译：哌嗪衍生物
公开(公告)号：US5169845A
公开(公告)日：1992-12-08
申请号：US768146
申请日：1991-09-30
申请人： Ian A. Cliffe , Graham J. Warrellow
发明人： Ian A. Cliffe , Graham J. Warrellow
IPC分类号： A61K31/415 , A61K31/44 , A61K31/4402 , A61K31/4409 , A61K31/4418 , A61K31/47 , A61K31/495 , A61K31/505 , A61P9/12 , A61P25/20 , A61P25/24 , A61P25/26 , C07D213/56 , C07D215/12 , C07D231/12 , C07D233/61 , C07D239/26 , C07D241/12 , C07D249/04 , C07D249/08 , C07D257/04 , C07D307/54 , C07D333/24 , C07D521/00
CPC分类号： C07D231/12 , C07D213/56 , C07D215/12 , C07D233/56 , C07D249/08 , C07D307/54 , C07D333/24
摘要： Piperazine derivative of formula ##STR1## and the pharmaceutically acceptable acid addition salts, where A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups, m is 0, 1 or 2, R is hydrogen or lower alkyl, R.sup.1 is aryl or a mono- or bicyclic heteroaryl radical, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is a heteroaryl radical, R.sup.4 is hydrogen, lower alkyl or aryl, and R.sup.5 is hydrogen, lower alkyl, cycloalkyl, cycloalkyl(lower)alkyl, aryl, or aryl(lower)alkyl or R.sup.4 and R.sup.5 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring which may contain a further hetero atom are 5--HT.sub.1A -binding agents and may be used, for example, as anxiolytics.

8. 发明授权

US5346896A 1-(aryl or heteroaryl)-4[.omega.-(aryl or heteroaryl).omega.-(aryl or heteroaryl)alkylene]piperazines 失效
标题翻译： 1-（芳基或杂芳基）-4 [ - （芳基或杂芳基）ω - （芳基或杂芳基）亚烷基]哌嗪
公开(公告)号：US5346896A
公开(公告)日：1994-09-13
申请号：US867221
申请日：1992-06-03
申请人： Terence J. Ward , Graham J. Warrellow
发明人： Terence J. Ward , Graham J. Warrellow
IPC分类号： A61K31/495 , A61P9/12 , A61P25/00 , A61P25/20 , A61P25/24 , A61P25/26 , A61P43/00 , C07D213/38 , C07D233/60 , C07D295/08 , C07D295/084 , C07D521/00 , C07D295/088 , C07D401/06 , C07D403/06
CPC分类号： C07D295/092 , C07D213/38 , C07D231/12 , C07D233/56 , C07D249/08
摘要： Disclosed herein are piperazine derivatives of the formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof, wherein W is (CH.sub.2).sub.m, CHOH or O,m is one of the integers 1 or 2,A is an alkylene chain of 1 to 3 carbon atoms optionally substituted by one or more (lower)alkyl groups,R is hydrogen or lower alkyl,R.sup.1 and R.sup.2 are each, independently, aryl or heteroaryl radicals with the proviso that R.sup.1 is not an optionally substituted indolyl radical,R.sup.3 is hydrogen or lower alkyl andR.sup.4 is an aryl or heteroaryl radical.The compounds are 5HT.sub.1A binding agents which may be used, for example, in the treatment of CNS disorders such as anxiety.
摘要翻译： PCT No.PCT / GB91 / 01693 Sec。 371日期：1992年6月3日 102（e）日期1992年6月3日PCT 1991年10月1日PCT PCT。公开号WO92 / 06082 日本公报1992年4月16日，公开的是式（I）的哌嗪衍生物或其药学上可接受的酸加成盐，其中W是（CH 2）m，CHOH或O，m是整数1或 2，A是任选被一个或多个（低级）烷基取代的具有1至3个碳原子的亚烷基链，R是氢或低级烷基，R 1和R 2各自独立地是芳基或杂芳基，条件是R 1是不是任选取代的吲哚基，R3是氢或低级烷基，R4是芳基或杂芳基。该化合物是5HT1A结合剂，其可用于例如治疗CNS疾病如焦虑症。

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