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1. 发明申请

WO1994010178A1 6-(SUBSTITUTED METHYLENE) PENEMS AND INTERMEDIATES 审中-公开
标题翻译： 6-（取代的甲基）基团和中间体
公开(公告)号：WO1994010178A1
公开(公告)日：1994-05-11
申请号：PCT/EP1993002894
申请日：1993-10-20
申请人： SMITHKLINE BEECHAM P L C , BROOM, Nigel, John, Perryman , HARRINGTON, Frank, Peter
发明人： SMITHKLINE BEECHAM P L C
IPC分类号： C07D519/00
CPC分类号： C07D513/04 , C07D233/90 , C07D499/88
摘要： Compounds of formula (I) in which: R is hydrogen or an organic substituent group; R is a fused bicyclic heterocyclic ring system of general formula (a) wherein R and R are independently hydrogen or one or more substituents replacing hydrogen atoms in the ring system shown; m is 2 or 3; p is 0, 1 or 2; and R is hydrogen, a salt-forming cation or an ester-forming group; and the symbol = / = indicates that the double bond may be in either the E or Z configuration.
摘要翻译：式（I）的化合物，其中：R 1是氢或有机取代基; R 2是通式（a）的稠合双环杂环体系，其中R 4和R 5独立地是氢或一个或多个取代所示环系中的氢原子的取代基; m为2或3; p为0,1或2; R 3是氢，成盐阳离子或成酯基; 符号= / =表示双键可以是E或Z配置。

2. 发明申请

WO9915526A3 N-5,6,7,8-TETRAHYDRO(1,6)NAPHTHYRIDINE-N'-PHENYLUREA DERIVATIVES 审中-公开
标题翻译： N-5,6,7,8-四氢呋喃（1,6）萘啶-N'-苯基衍生物
公开(公告)号：WO9915526A3
公开(公告)日：1999-05-20
申请号：PCT/EP9805904
申请日：1998-09-15
申请人： SMITHKLINE BEECHAM PLC , HARRINGTON FRANK PETER , THOMPSON MERVYN
发明人： HARRINGTON FRANK PETER , THOMPSON MERVYN
IPC分类号： A61K31/4375 , A61P9/00 , A61P25/00 , A61P25/04 , A61P25/06 , A61P25/08 , A61P25/14 , A61P25/16 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , A61P43/00 , C07D471/04 , A61K31/445
CPC分类号： C07D471/04
摘要： N-(naphthyridinyl)-N'-phenyl-ureas/thioureas of general formula (I) are useful for the treatment and/or prophylaxis of anxiety, mania, depression, panic disorders and/or aggression, disorders associated with a subarachnoid haemorrhage or neural shock, the effects associated with withdrawal from substances of abuse such as cocaine, nicotine, alcohol and benzodiazepines, disorders treatable and/or preventable with anti-convulsive agents, such as epilepsy including post-traumatic epilepsy, Parkinson's disease, psychosis, migraine, cerebral ischaemia, Alzheimer's disease and other degenerative diseases such as Huntingdon's chorea, schizophrenia, obsessive compulsive disorders (OCD), neurological deficits associated with AIDS, sleep disorders (including circadian rhythm disorders, insomnia and narcolepsy), tics (e.g. Giles de la Tourette's syndrome), traumatic brain injury, tinnitus, neuralgia, especially trigeminal neuralgia, neuropathic pain, dental pain, cancer pain, inappropriate neuronal activity resulting in neurodysthesias in diseases such as diabetes, multiple sclerosis (MS) and motor neurone disease, ataxias, muscular rigidity (spasticity), temporomandibular joint dysfunction, and amyotrophic lateral sclerosis (ALS).
摘要翻译：通式（I）的N-（二氮杂吖啶基）-N'-苯基 - 脲/硫脲可用于治疗和/或预防焦虑症，躁狂症，抑郁症，惊恐障碍和/或侵略，与蛛网膜下腔出血相关的疾病或神经性休克，与诸如可卡因，尼古丁，酒精和苯并二氮杂类药物的滥用物质相关的作用，可用抗惊厥药物治疗和/或预防的疾病，如癫痫，包括创伤后癫痫，帕金森病，精神病，偏头痛，脑缺血，阿尔茨海默病和其他退行性疾病如亨廷顿舞蹈病，精神分裂症，强迫症（OCD），与艾滋病相关的神经功能缺陷，睡眠障碍（包括昼夜节律紊乱，失眠和发作性睡眠），抽搐（如Giles de la Tourette综合征），创伤性脑损伤，耳鸣，神经痛，特别是三叉神经痛，神经性疼痛，牙痛，癌症疼痛，不适当的神经元导致糖尿病，多发性硬化（MS）和运动神经元疾病，共济失调，肌肉僵硬（痉挛），颞下颌关节功能障碍和肌萎缩性侧索硬化（ALS）等疾病中的神经损伤的活动。

3. 发明申请

WO2003068772A1 HETEROCYCLIC COMPOUNDS POSSESSING AFFINITY AT 5HT1-TYPE RECEPTORS AND USE THEREOF IN THERAPY 审中-公开
标题翻译：在5HT1型受体上具有重要性的杂环化合物及其在治疗中的应用
公开(公告)号：WO2003068772A1
公开(公告)日：2003-08-21
申请号：PCT/EP2003/001711
申请日：2003-02-17
申请人： GLAXO GROUP LIMITED , HARRINGTON, Frank, Peter , SMITH, Paul, William , WARD, Simon, E
发明人： HARRINGTON, Frank, Peter , SMITH, Paul, William , WARD, Simon, E
IPC分类号： C07D413/12
CPC分类号： C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof are disclosed:(I)wherein A is optionally substituted phenyl, naphthyl, indolyl, quinolinyl, quinazolinyl, indazolyl, isoquinolinyl or benzofuranyl; b is 1, 2 or 3 and c is 1, 2 or 3, wherein b + c is 2, 3, 4 or 5; X is carbon, Y is CH, is a double bond and e is 0; or X is carbon, Y is CH2 or oxygen, is a single bond and e is 1; or X is nitrogen, Y is CH2, is a single bond and e is 0; R1 is hydrogen, cyano, halogen, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, NHCOCH3 or OCONR5R6, wherein R5 and R6 are independently hydrogen or C1-6alkyl; R2 is halogen, cyano or C1-6alkoxy; d is 0, 1, 2 or 3; R3 is hydrogen, C1-6alkyl, C1-6alkanoyl, fluoroC1-6alkanoyl, C1-6alkylsulfonyl, fluoroC1-6alkylsulfonyl, carbamoyl, C1-6alkylcarbamoyl or arylC1-6alkyl; and R4, together with the nitrogen atom to which it is attached, forms an optionally substituted 5 to 7 membered heterocyclic group fused to the benzene ring, provided that when a compound of formula (I) has the following structure: wherein A, b, c, R1, e, X, Y, R2 and d are as defined above and R3 is hydrogen, C1-6alkyl or arylC1-6alkyl, then (i) X is carbon, Y is CH and is a double bond; or (ii) b and c are both 1; or (iii) the carbon atom adjacent to the oxo-substituted carbon atom in the morpholinyl ring, marked " * ", is substituted. Methods of preparing the compounds and uses of the compounds in therapy, in particular for a CNS disorder such as depression or anxiety, are also disclosed.
摘要翻译：公开了式（I）化合物及其药学上可接受的盐：（I）其中A是任选取代的苯基，萘基，吲哚基，喹啉基，喹唑啉基，吲唑基，异喹啉基或苯并呋喃基; b为1,2或3，c为1,2或3，其中b + c为2,3,4或5; X是碳，Y是CH，是双键，e是0; 或X为碳，Y为CH 2或氧，为单键，e为1; 或X是氮，Y是CH 2，是单键，e是0; R 1是氢，氰基，卤素，C 1-6烷基，C 1-6烷氧基，C 1-6烷氧基C 1-6烷基，NHCOCH 3或OCONR 5 R 6，其中R 5和R 6独立地是氢或C 1-6烷基; R2是卤素，氰基或C1-6烷氧基; d为0,1,2或3; R 3是氢，C 1-6烷基，C 1-6烷酰基，氟C 1-6烷酰基，C 1-6烷基磺酰基，氟C 1-6烷基磺酰基，氨基甲酰基，C 1-6烷基氨基甲酰基或芳基C 1-6烷基; 并且R 4与其所连接的氮原子一起形成与苯环稠合的任选取代的5至7元杂环基，条件是当式（I）化合物具有以下结构时：其中A，b， c，R1，e，X，Y，R2和d如上定义，R3是氢，C1-6烷基或芳基C1-6烷基，则（i）X是碳，Y是CH并且是双键; 或（ii）b和c均为1; 或（iii）标记为“*”的吗啉基环上与氧代取代的碳原子相邻的碳原子被取代。还公开了制备化合物的方法和化合物在治疗中的用途，特别是用于CNS障碍如抑郁或焦虑的用途。

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