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1. 发明授权

US4921958A Piperazinylalkylcarboxylic acid adamantylamides 失效
标题翻译：哌嗪基烷基羧酸金刚烷基酰胺
公开(公告)号：US4921958A
公开(公告)日：1990-05-01
申请号：US413407
申请日：1989-09-27
申请人： Magid A. Abou-Gharbia , John P. Yardley , Wayne E. Childers, Jr. , Ian A. Cliffe
发明人： Magid A. Abou-Gharbia , John P. Yardley , Wayne E. Childers, Jr. , Ian A. Cliffe
IPC分类号： C07D239/42 , C07D295/13 , C07D295/15
CPC分类号： C07D295/13 , C07D239/42 , C07D295/15
摘要： The compounds of the formula: ##STR1## wherein Ad is 1-adamantyl, 2-adamantyl or 3-noradamantyl; n is 1,2,3,4 or 5; R.sup.1 hydrogen, alkyl, phenyl, benzyl, or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, cyano, nitro or trifluoromethyl; R.sup.2 is phenyl, benzyl or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhalomethyl, 2-, 3-, or 4-pyridinyl, 2-, 4- or 5-pyrimidinyl or 2- or 3-pyrazinyl; R.sup.3 and R.sup.4 are, independently, hydrogen, methyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof, are useful anxiolytic/antidepressant agents, with elements of antipsychotic activity.
摘要翻译：下式的化合物：其中Ad是1-金刚烷基，2-金刚烷基或3-降金刚烷基; n为1,2,3,4或5; 烷基，苯基，苄基或取代的苯基或苄基，其中取代基是烷基，烷氧基，卤素，氰基，硝基或三氟甲基; R2是苯基，苄基或取代的苯基或苄基，其中取代基是烷基，烷氧基，卤素，硝基，氰基或全卤代甲基，2-，3-或4-吡啶基，2-，4-或5-嘧啶基或2- 或3-吡嗪基; R 3和R 4独立地是氢，甲基，苯基或苄基; 或其药学上可接受的盐是具有抗精神病活性成分的抗焦虑/抗抑郁药。

2. 发明授权

US4988814A Tertiary alkyl functionalized piperazine derivatives 失效
标题翻译：叔烷基官能化哌嗪衍生物
公开(公告)号：US4988814A
公开(公告)日：1991-01-29
申请号：US428148
申请日：1989-10-27
申请人： Magid A. Abou-Gharbia , John P. Yardley , Ian A. Cliffe
发明人： Magid A. Abou-Gharbia , John P. Yardley , Ian A. Cliffe
IPC分类号： C07D239/42 , C07D295/13 , C07D295/15
CPC分类号： C07D295/13 , C07D239/42 , C07D295/15
摘要： Compounds of the formula: ##STR1## in which R.sup.1 is alkyl; R.sup.2 and R.sup.3 are alkyl or taken together they are polymethylene, R.sup.2 and R.sup.3 complete a 5-norbornen-2-yl moiety; X is --CO.sub.2 --, --OCO--, --OCO.sub.2 --, --N(R.sup.7)CO--, --NHNHCO--, --ON(R.sup.7)CO--, --CON(R.sup.7)--, --N(R.sup.7)CO.sub.2 --, --OCON(R.sup.7)-- or --N(R.sup.7)CON(R.sup.8)--, wherein R.sup.7 and R.sup.8 are, independently, hydrogen, alkyl, phenyl, benzyl, substituted phenyl or substituted benzyl in which the substituents are halo, alkyl alkoxy, cyano, nitro or perhalomethyl; R.sup.4 is hydrogen or alkyl; R.sup.5 is hydrogen, alkyl, hydroxyalkyl, phenyl, benzyl, substituted phenyl or substituted benzyl in which the substituents are hydroxy, halo, alkyl alkoxy, trifluoromethyl, nitro, cyano, carbalkoxy, carboxamido, amino, alkylamino or dialkylamino; R.sup.6 is phenyl, benzyl, 2-, 3-, or 4-pyridinyl, 2-pyrimidinyl or 2-pyrazinyl any of which may be substituted by one or more hydroxy, halo, alkyl alkoxy, trifluoromethyl, nitro, cyano, carbalkoxy, carboxamido, amino, alkylamino or dialkylamino; n is one of the integers 0, 1, 2, 3, 4 or 5; or a pharmaceutically acceptable salt thereof, with the proviso that when X is --CON(R.sup.7)-- and R.sup.7 is alkyl, R.sup.6 is other than 2-pyrimidinyl, and when X is --CO.sub.2 -- and R.sup.1, R.sup.2 and R.sup.3 are methyl and n is 1, R.sup.6 is other than 3,5-di(trifluoromethyl)phenyl are antidepressant and/or anxiolytic agents.

3. 发明授权

US5610154A Bicyclic carboxamides 失效
标题翻译：双环甲酰胺
公开(公告)号：US5610154A
公开(公告)日：1997-03-11
申请号：US448962
申请日：1995-05-24
申请人： Ian A. Cliffe , Howard L. Mansell , Terence J. Ward , James A. Nelson , Uresh S. Shah , Mira A. Kanzelberger
发明人： Ian A. Cliffe , Howard L. Mansell , Terence J. Ward , James A. Nelson , Uresh S. Shah , Mira A. Kanzelberger
IPC分类号： A61K31/495 , A61K31/55 , A61P9/12 , A61P25/18 , A61P25/20 , A61P43/00 , C07D209/44 , C07D209/52 , C07D223/14 , C07D295/185 , C07D403/12 , C07D451/02 , C07D295/16
CPC分类号： C07D295/185 , C07D209/52 , C07D223/14 , C07D451/02
摘要： Bicyclic carboxamides of formula I ##STR1## and the pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents, particularly 5-HT.sub.1A antagonists and may be used, for example, as anxiolytics. In the formulaX represents --CR.sup.2 .dbd.CR.sup.2 -- or --(CR.sup.2)q--;m represents 0,1 or 2; n represents 0,1 or 2; p represents 0,1,2 or 3 and q represents 0,1,2 or 3;A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups,R is a mono or bicyclic aryl or heteroaryl radical,R.sup.1 is an aryl or aryl(lower)alkyl radicaland each R.sup.2 is independently hydrogen or lower alkyl.
摘要翻译：式I的双环甲酰胺（I）和药学上可接受的酸加成盐是5-HT1A结合剂，特别是5-HT 1A拮抗剂，并且可以用于例如抗焦虑剂。式X表示-CR2 = CR2-或 - （CR2）q-; m表示0,1或2; n表示0,1或2; p表示0,1,2或3，q表示0,1,2或3; A是任选被一个或多个低级烷基取代的1或2个碳原子的亚烷基链，R是单或双环芳基或杂芳基，R 1是芳基或芳基（低级）烷基，每个R 2独立地是氢或低级烷基。

4. 发明授权

US5369103A Piperazine derivatives 失效
标题翻译：哌嗪衍生物
公开(公告)号：US5369103A
公开(公告)日：1994-11-29
申请号：US861834
申请日：1992-06-19
申请人： Ian A. Cliffe , Alan C. White , Anderson D. Ifill
发明人： Ian A. Cliffe , Alan C. White , Anderson D. Ifill
IPC分类号： A61K31/495 , A61P9/12 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/26 , A61P43/00 , C07D213/56 , C07D295/14 , C07D295/18 , C07D295/185 , A61K31/395 , C07D403/06 , C07D403/14
CPC分类号： C07D295/185 , C07D213/56
摘要： ##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
1 is a mono or bicyclic aryl or a heteroaryl radical, R
2 is an aryl radical, a heteroaryl radical, or an aryl-or heteroaryl-lower alkyl radical, R
3 is hydrogen, lower alkyl or aryl and R
4 is hydrogen, lower alkyl, cycloalkyl, cycloalkyl(lower)alkyl, aryl, or aryl(lower)alkyl or R
3 and R
4 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring which may contain a further hetero atom and the dotted line represents a single or double bond, the hydrogen atoms shown in brackets being present when the dotted line represents a single bond and their pharmaceutically acceptable acid addition salts are 5-HT
1A binding agents which may be used, for example, for the treatment of CNS disorders such as anxiety.
摘要翻译：（I）其中A是任选被一个或多个低级烷基取代的1或2个碳原子的亚烷基链，R是氢或低级烷基，R 1是单或双环芳基或杂芳基，R 2是芳基，芳基或杂芳基 - 低级烷基，R3是氢，低级烷基或芳基，R4是氢，低级烷基，环烷基，环烷基（低级）烷基，芳基或芳基（低级）烷基或者R 3和R 4与它们所连接的氮原子一起表示饱和杂环，其可以含有另外的杂原子，虚线表示单键或双键，当虚线表示时，括号中所示的氢原子存在代表单键，并且其药学上可接受的酸加成盐是可用于例如治疗CNS病症如焦虑症的5-HT1A结合剂。

5. 发明授权

US5194439A N-(2,3-dihydro-1,4-benzodioxinyl)-N-substituted aminopyrido-fused cycloalkanes 失效
标题翻译： N-（2,3-二氢-1,4-苯并二恶英基）-N-取代的氨基吡啶并 - 稠合的环烷烃
公开(公告)号：US5194439A
公开(公告)日：1993-03-16
申请号：US765282
申请日：1991-09-25
申请人： Ian A. Cliffe , Howard L. Mansell , Richard S. Todd , Alan C. White
发明人： Ian A. Cliffe , Howard L. Mansell , Richard S. Todd , Alan C. White
IPC分类号： C07D215/38 , C07D405/12
CPC分类号： C07D405/12 , C07D215/38
摘要： Pyridine derivatives of formula ##STR1## their heteroaromatic N-oxides and their pharmaceutically acceptable acid addition salts are disclosed. In the formula z is 0, 1 and 2; R is hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, trifluoromethyl, nitro, amino, (lower)alkylamino or di(lower)alkylamino; R.sup.1 is hydrogen or lower alkyl; R.sup.2 is --(CH.sub.2).sub.n --R.sup.3 or --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.m --R.sup.3 or --CH.sub.2.C.tbd.C.(CH.sub.2).sub.m --R.sup.3 where n is 1 to 6, and m is 0 to 3; and R.sup.3 is a ring of formula ##STR2## The compounds exhibit activity as 5-HT.sub.1A agonists, antagonists or partial agonists and are used for the treatment of CNS disorders, e.g. anxiety, as antihypertensives and in treating anorexia.
摘要翻译：公开了式（I）的吡啶衍生物，它们的杂芳族N-氧化物及其药学上可接受的酸加成盐。式中Z为0,1和2; R为氢，羟基，低级烷基，低级烷氧基，卤素，三氟甲基，硝基，氨基，（低级）烷基氨基或二（低级）烷基氨基; R1是氢或低级烷基; R 2是 - （CH 2）n -R 3或-CH 2 -CH = CH-（CH 2）m -R 3或-CH 2 C 3 OCH 3（CH 2）m -R 3，其中n为1至6，m为0至3 ; 并且R 3是式的环。化合物表现出作为5-HT 1A激动剂，拮抗剂或部分激动剂的活性，并且用于治疗CNS疾病，例如，焦虑，作为抗高血压药物和治疗厌食症。

6. 发明授权

US4784996A Pyrimidoindoles useful as hypoglycaemics 失效
标题翻译：嘧啶二醇可用作低血糖症
公开(公告)号：US4784996A
公开(公告)日：1988-11-15
申请号：US23337
申请日：1987-03-09
申请人： Alan C. White , Ian A. Cliffe , Richard S. Todd
发明人： Alan C. White , Ian A. Cliffe , Richard S. Todd
IPC分类号： C07D487/04 , A61K31/505
CPC分类号： C07D487/04
摘要： Compounds of formula ##STR1## wherein A represents a lower alkylene chain optionally containing one double or triple bond, RO represents (lower)alkoxy, aryl(lower)alkoxy, hydroxy or protected hydroxy, R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower)alkylamino and R.sup.3 and R.sup.4 each independently represent hydrogen or lower alkyl and their pharmaceutically acceptable acid addition salts are useful as hypoglycaemics or as intermediates for hypoglycaemics.
摘要翻译：式（I）的化合物其中A表示任选含有一个双键或三键的低级亚烷基链，RO表示（低级）烷氧基，芳基（低级）烷氧基，羟基或被保护的羟基，R 1和R 2可以相同或各自代表氢，羟基，低级烷基，低级烷氧基，卤代（低级）烷基，卤素，氨基或单或二（低级）烷基氨基，并且R 3和R 4各自独立地表示氢或低级烷基及其药学上可接受的酸加成盐作为低血糖症或低血糖症的中间体是有用的。

7. 发明申请

US20110166088A1 BENZOTHIAZOLES AND AZA-ANALOGUES THEREOF USE AS ANTIBACTERIAL AGENTS 审中-公开
标题翻译：苯并噻唑类及其类似物作为抗菌剂使用
公开(公告)号：US20110166088A1
公开(公告)日：2011-07-07
申请号：US13000561
申请日：2009-06-25
申请人： Jitendra A. Sattigeri , Naresh Kumar , Ajay Yadav , Lalima Sharma , Ian A. Cliffe , Shibu B. Varughese , Shaikh Rizwan Shabbir , V. Samuel Raj , Dilip J. Upadhyay , Pradip K. Bhatnager
发明人： Jitendra A. Sattigeri , Naresh Kumar , Ajay Yadav , Lalima Sharma , Ian A. Cliffe , Shibu B. Varughese , Shaikh Rizwan Shabbir , V. Samuel Raj , Dilip J. Upadhyay , Pradip K. Bhatnager
IPC分类号： A61K31/7068 , C07D417/14 , C07D413/14 , C07H17/02 , A61K31/444 , A61K31/4439 , A61K31/496 , A61K31/5355 , A61K31/513 , A61K31/506 , A61P31/04
CPC分类号： C07D417/14 , C07D417/04 , C07D493/04
摘要： The present invention provides Gyrase B and/or Topoisomerase IV par E inhibitors, which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, Staphylococci, Streptococci, Enterococci, Haemophilus, Pseudomonas spp., Acenetobacter spp., Moraxalla spp., Chlamydia spp., Mycoplasma spp., Legionella spp., Ktycobacterium spp., Helicobacter, Clostridium spp., Bacteroides spp., Corynebacterium, Bacillus spp., Enterobactericeae,’ (E. coli, Klebsiella spp., Proteus spp., etc.) or any combination thereof. Also provided, are processes for preparing compounds disclosed herein, pharmaceutical compositions containing compounds disclosed herein, and methods of treating bacterial infections. (Formula)
摘要翻译：本发明提供可用作抗菌剂的促旋酶B和/或拓扑异构酶IV对E抑制剂。本文公开的化合物可用于治疗或预防由革兰氏阳性，革兰氏阴性和厌氧细菌引起的或由其贡献的病症，更具体地针对例如葡萄球菌，链球菌，肠球菌，嗜血杆菌，假单胞菌属，醋酸杆菌属，莫氏假单胞菌，衣原体属（Chlamydia spp。），支原体属（Mycoplasma spp。），军团菌属（Legionella spp。），科分枝杆菌属（Ktycobacterium spp。），幽门螺杆菌属（Helicobacter），梭菌属（Clostridium spp。），拟杆菌属（Bacteroides spp。），棒杆菌属（Corynebacterium），芽孢杆菌属（Bacillus spp。），肠杆菌属（Enterobactersisae），（E.coli，Klebsiella spp。，Proteus spp。等等）或其任何组合。还提供了制备本文公开的化合物的方法，含有本文公开的化合物的药物组合物，以及治疗细菌感染的方法。（式）

8. 发明授权

US07041683B2 Antidepressant azaheterocyclylmethyl derivatives of 2,3-dihydro-1, 4-benzodiozan 失效
标题翻译： 2,3-二氢-1,4-苯并二氮杂的抗抑郁药氮杂环甲基衍生物
公开(公告)号：US07041683B2
公开(公告)日：2006-05-09
申请号：US10390478
申请日：2003-03-17
申请人： George E. M. Husbands , Gary P. Stack , Richard E. Mewshaw , Ian A. Cliffe
发明人： George E. M. Husbands , Gary P. Stack , Richard E. Mewshaw , Ian A. Cliffe
IPC分类号： A01N43/40 , A61K31/44
CPC分类号： C07D405/14 , C07D471/04
摘要： Compounds of the formula useful for the treatment of depression and other conditions such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, sexual dysfunction, eating disorders, addictive disorders caused by ethanol or cocaine abuse and related illnesses.
摘要翻译：可用于治疗抑郁症和其他疾病如强迫症，恐慌发作，广泛性焦虑症，性功能障碍，饮食失调，乙醇或可卡因滥用引起的成瘾性疾病和相关疾病的化合物。

9. 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.

10. 发明授权

US5075303A Pyridine derivatives 失效
公开(公告)号：US5075303A
公开(公告)日：1991-12-24
申请号：US505957
申请日：1990-04-06
申请人： Ian A. Cliffe , Howard L. Mansell , Richard S. Todd , Alan C. White
发明人： Ian A. Cliffe , Howard L. Mansell , Richard S. Todd , Alan C. White
IPC分类号： A61K31/00 , A61K31/435 , A61K31/47 , A61K31/4709 , A61K31/473 , A61P43/00 , C07D215/38 , C07D221/04 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12 , C07D417/12 , C07D513/04
CPC分类号： C07D401/12 , C07D215/38 , C07D405/12
摘要： Pyridine derivatives of formula ##STR1## their heteroaromatic N-oxides and their pharmaceutically acceptable acid addition salts are disclosed. In the formula z is 0, 1 and 2 and R, R.sup.1, R.sup.2 and R.sup.2 have specified meanings. The compounds exhibit activity as 5-HT.sub.1A agonists, antagonists or partial agonists and are useful for the treatment of CNS disorders e.g. anxiety, as antihypertensives and in treating anorexia.

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