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1. 发明申请

WO1994029277A1 AMILINO- OR PYRIDYLAMINO- CYCLOBUTENE- 1,2-DIONE DERIVATIVES AS cGMP PHOSPHODIESTERASE INHIBITORS 审中-公开
标题翻译：作为cGMP磷酸二酯酶抑制剂的AMILINO-或PYRIDYLAMINO-CYCLOBUTENE-1,2-二酮衍生物
公开(公告)号：WO1994029277A1
公开(公告)日：1994-12-22
申请号：PCT/EP1994001921
申请日：1994-06-07
申请人： SMITHKLINE BEECHAM PLC , COATES, William, John , RAWLINGS, Derek, Anthony
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D233/38
CPC分类号： C07D213/74 , C07C225/20 , C07C2601/04 , C07D209/14 , C07D213/38 , C07D213/65 , C07D233/24 , C07D235/18 , C07D239/26 , C07D263/32 , C07D263/57 , C07D333/20 , C07D335/08
摘要： A compound of formula (1) or a pharmaceutically acceptable salt thereof, wherein Ar is an optionally substituted aryl or heteroaryl ring selected from phenyl, naphthyl, pyridyl, pyrimidyl, pyridazinyl, pyrazinyl, imidazolyl, thienyl, oxazolyl, benzimidazolyl, benzoxazolyl, indolyl or thianaphthenyl, X is CH or N; R is NR R or hydrogen; and R and R are independently hydrogen or C1-6alkyl. The compounds of this invention are inhibitors of calmodulin insensitive cyclic GMP phosphodiesterase and are of use in combating such conditions where such inhibition is thought to be beneficial.
摘要翻译：式（1）化合物或其药学上可接受的盐，其中Ar是任选取代的芳基或杂芳基环，其选自苯基，萘基，吡啶基，嘧啶基，哒嗪基，吡嗪基，咪唑基，噻吩基，恶唑基，苯并咪唑基，苯并恶唑基，吲哚基或噻吩并苯基，X为CH或N; R 0是NR 1 R 2或氢; R 1和R 2独立地是氢或C 1-6烷基。本发明的化合物是钙调蛋白不敏感的环状GMP磷酸二酯酶的抑制剂，并且用于对抗这种抑制被认为是有益的这种状况。

2. 发明申请

WO1994014771A1 TRYPTAMINE ANALOGUES AS 5-HT1-LIKE AGONISTS 审中-公开
标题翻译：作为5-HT1型激动剂的三甲酚胺类似物
公开(公告)号：WO1994014771A1
公开(公告)日：1994-07-07
申请号：PCT/EP1993003564
申请日：1993-12-14
申请人： SMITHKLINE BEECHAM PLC , PORTER, Roderick, Alan , COATES, William, John
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D209/16
CPC分类号： C07D401/04 , C07D209/14 , C07D209/16 , C07D401/14 , C07D403/04
摘要： A compound of structure (I), in which R is an optionally substituted 6- to 10-membered aryl or heteroaryl ring; suitably R is an optionally substituted 6- or 10-membered aryl ring such as phenyl or naphthyl; suitably R is an optionally substituted 6- to 10-membered heteroaryl ring containing from 1 to 4 nitrogen atoms. R is hydrogen, halogen, C1-4 alkyl, CN, NO2 or CF3; R is hydrogen, halogen, C1-4 alkyl, CN, NO2 or CF3; R is C(R )(R )CH2NR R , -CH = NNHC(NH)NH2 or a; R and R are independently hydrogen or C1-4 alkyl; R and R are the same or different and are each hydrogen or C1-4 alkyl or together with the nitrogen atom to which they are attached form a ring; R is hydrogen, C1-4 alkyl, or C3-6 alkenyl; R is hydrogen and R is hydrogen or hydroxy, or R and R together represent a bond; and q and m are independently 1 or 2; and pharmaceutically acceptable salts, solvates and hydrates thereof. The compounds are 5-HT1-like agonists (or partial agonists) and as such are expected to have utility in medicine in the treatment and/or prophylaxis of migraine, and other conditions associated with cephalic pain, such as cluster headache, headache associated with vascular disorders and other neuralgia. They are also expected to have utility in the treatment or prophylaxis of portal hypertension.
摘要翻译：结构（I）的化合物，其中R 1是任选取代的6至10元芳基或杂芳基环; 合适的R 1是任选取代的6-或10-元芳环，例如苯基或萘基; 适当地，R 1是含有1至4个氮原子的任选取代的6至10元杂芳基环。 R 2是氢，卤素，C 1-4烷基，CN，NO 2或CF 3; R 3是氢，卤素，C 1-4烷基，CN，NO 2或CF 3; R 3是C（R 4）（R 5）CH 2 NR 6 R 7，-CH = NNHC（NH）NH 2或a; R 4和R 5独立地是氢或C 1-4烷基; R 6和R 7相同或不同，各自为氢或C 1-4烷基，或与它们所连接的氮原子一起形成环; R 8是氢，C 1-4烷基或C 3-6烯基; R a是氢，R b是氢或羟基，或R a和R b一起表示键; q和m独立地为1或2; 及其药学上可接受的盐，溶剂化物和水合物。化合物是5-HT1样激动剂（或部分激动剂），因此预期在医学中可用于治疗和/或预防偏头痛以及与头痛相关的其它病症，例如丛集性头痛，与头痛相关的头痛血管疾病等神经痛。它们也预期可用于治疗或预防门静脉高压。

3. 发明申请

WO1998055139A1 USE OF LEPTIN ANTAGONISTS FOR THE TREATMENT OF DIABETES 审中-公开
标题翻译：使用LEPTIN拮抗剂治疗糖尿病
公开(公告)号：WO1998055139A1
公开(公告)日：1998-12-10
申请号：PCT/EP1997002240
申请日：1997-06-06
申请人： SMITHKLINE BEECHAM PLC , CAWTHORNE, Michael, Anthony , EMILSSON, Valur , LIU, Yong-Ling
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： A61K38/22
CPC分类号： C07K16/28 , A61K38/2264
摘要： The use of an antagonist of leptin for the manufacture of a medicament for the treatment of disorders resulting from deficiencies in insulin secretion, hyperglycaemia and insulin resistance.
摘要翻译：瘦素拮抗剂用于制备用于治疗由胰岛素分泌不足，高血糖症和胰岛素抵抗引起的疾病的药物的用途。

4. 发明申请

WO1998028311A1 PHARMACEUTICAL AMINOPHOSPHONIC ACID DERIVATIVES 审中-公开
标题翻译：药物氨基膦酸衍生物
公开(公告)号：WO1998028311A1
公开(公告)日：1998-07-02
申请号：PCT/EP1997007192
申请日：1997-12-17
申请人： SYMPHAR S.A. , SMITHKLINE BEECHAM PLC , NGUYEN, Lan, Mong , PHAN, Hieu, Trung , VAN DIEP, Vinh , FLORET, Simon , CHRISTINAT, Alexia , NIESOR, Eric , BENTZEN, Craig, Leigh , IFE, Robert, John
发明人： SYMPHAR S.A. , SMITHKLINE BEECHAM PLC
IPC分类号： C07F09/58
CPC分类号： C07F9/58
摘要： Aminophosphonates alpha substituted by phenol groups, of formula (I) have lipoprotein(a) lowering activity.
摘要翻译：本发明涉及由式（I）表示的苯酚取代的α-氨基膦酸酯，其具有倾向于降低脂蛋白（a）水平的活性。

5. 发明申请

WO1998014461A1 NOVEL spsB 审中-公开
公开(公告)号：WO1998014461A1
公开(公告)日：1998-04-09
申请号：PCT/US1997017678
申请日：1997-09-30
申请人： SMITHKLINE BEECHAM PLC , BLACK, Michael, T. , O'DWYER, Karen, M.
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07H21/02
CPC分类号： C07K14/31 , A61K38/00 , A61K39/00 , A61K48/00 , C12N9/52
摘要： spsB polypeptides and DNA (RNA) encoding such spsB and a procedure for producing such polypeptides by recombinant techniques is disclosed. Also disclosed are methods for utilizing such spsB for the treatment of infection, particularly bacterial infections. Antagonists against such spsB and their use as a therapeutic to treat infections, particularly bacterial infections are also disclosed. Also disclosed are diagnostic assays for detecting diseases related to the presence of spsB nucleic acid sequences and the polypeptides in a host. Also disclosed are diagnostic assays for detecting polynucleotides encoding spsB and for detecting the polypeptide in a host.
摘要翻译：公开了spsB多肽和编码这种spsB的DNA（RNA）和通过重组技术产生这种多肽的方法。还公开了利用这种spsB来治疗感染，特别是细菌感染的方法。还公开了抗这种spsB的拮抗剂及其用作治疗感染，特别是细菌感染的治疗剂。还公开了用于检测与宿主中spsB核酸序列和多肽的存在相关的疾病的诊断测定法。还公开了用于检测编码spsB的多核苷酸并用于检测宿主中的多肽的诊断测定。

6. 发明申请

WO1998006718A1 PROCESS FOR THE PREPARATION OF BENZOPYRAN COMPOUNDS 审中-公开
标题翻译：制备苯并噻唑化合物的方法
公开(公告)号：WO1998006718A1
公开(公告)日：1998-02-19
申请号：PCT/EP1997004328
申请日：1997-08-05
申请人： SMITHKLINE BEECHAM PLC , GILES, Robert, Gordon , OXLEY, Paul
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D405/04
CPC分类号： C07D405/04 , C07C231/10 , C07C233/80
摘要： A process for preparing certain substituted benzopyran compounds is disclosed.
摘要翻译：公开了制备某些取代的苯并吡喃化合物的方法。

7. 发明申请

WO1998004258A1 FORMULATION FOR THE TREATMENT AND/OR PROPHYLAXIS OF DEMENTIA 审中-公开
标题翻译：治疗和/或预防的方法的配方
公开(公告)号：WO1998004258A1
公开(公告)日：1998-02-05
申请号：PCT/EP1997003872
申请日：1997-07-14
申请人： SMITHKLINE BEECHAM PLC , VAN-SCHIE, Dirk, Marinus, Johannes
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： A61K31/435
CPC分类号： A61K9/7084 , A61K31/439
摘要： A pharmaceutical composition for administration to the skin, which comprises [R-(Z)]- alpha -(methoxyimino)- alpha -(1-azabicyclo [2.2.2]oct-3-yl)acetonitrile or a pharmaceutically acceptable salt thereof together with a suitable pharmaceutically acceptable carrier, for the treatment or prophylaxis of dementia.
摘要翻译：含有[R-（Z）]-α-（甲氧基亚氨基）-α-（1-氮杂双环[2.2.2]辛-3-基）乙腈或其药学上可接受的盐的皮肤给药用药物组合物与合适的药学上可接受的载体，用于治疗或预防痴呆。

8. 发明申请

WO1997048699A1 INDOLINE DERIVATIVES USEFUL AS 5-HT-2C RECEPTOR ANTAGONISTS 审中-公开
标题翻译：吲哚衍生物作为5-HT-2C受体拮抗剂有用
公开(公告)号：WO1997048699A1
公开(公告)日：1997-12-24
申请号：PCT/EP1997003156
申请日：1997-06-16
申请人： SMITHKLINE BEECHAM PLC , BROMIDGE, Steven, Mark , FORBES, Ian, Thomson
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D401/14
CPC分类号： C07D401/14
摘要： The invention relates to heterocyclic compounds of formula (I) or a salt thereof wherein X is CH or N; R is hydrogen or C1-6 alkyl; R and R groups are independently halogen, C1-6 alkyl, or trifluoromethyl, having pharmacological activity, processes for their preparation, to compositions containing them and to their use in the treatment of CNS disorders such as anxiety.
摘要翻译：本发明涉及式（I）的杂环化合物或其盐，其中X为CH或N; R 1是氢或C 1-6烷基; R 2和R 3基团独立地是具有药理学活性的卤素，C 1-6烷基或三氟甲基，其制备方法，含有它们的组合物以及它们在治疗CNS疾病如焦虑症中的应用。

9. 发明申请

WO1997048681A1 SULPHONAMIDE DERIVATIVES AND THEIR USE IN THE TREATMENT OF CNS DISORDERS 审中-公开
标题翻译：磺酰胺衍生物及其在治疗CNS病症中的应用
公开(公告)号：WO1997048681A1
公开(公告)日：1997-12-24
申请号：PCT/EP1997003159
申请日：1997-06-17
申请人： SMITHKLINE BEECHAM PLC , FORBES, Ian, Thomson , KING, Francis, David , RAHMAN, Shirley, Katherine
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D211/26
CPC分类号： C07D451/02 , C07D207/48 , C07D211/96 , C07D221/24 , C07D223/04 , C07D279/12 , C07D401/06 , C07D401/12 , C07D409/12 , C07D451/06
摘要： Sulphonamide compounds of formula (I) or a salt thereof, wherein: Ar is an optionally substituted mono- or bicyclic aromatic or heteroaromatic ring; R and R are independently hydrogen, C1-6 alkyl, arylC1-6 alkyl or together with the nitrogen atom to which they are attached form an optionally substituted 5- to 7-membered heterocyclic ring optionally containing a further heteroatom selected from nitrogen, sulphur or oxygen, the nitrogen atom being substituted by hydrogen, C1-6 alkyl, cycloC3-7alkyl, or an optionally substituted aryl, heteroaryl or arylC1-6 alkyl group; R is hydrogen or C1-6 alkyl; X is oxygen, sulphur or a bond; n is 2 or 3; and m is 1 or 2, having pharmacological activity, processes for their preparation, compositions containing them and their use in the treatment of CNS disorders.
摘要翻译：式（I）的磺酰胺化合物或其盐，其中：Ar是任选取代的单环或双环芳族或杂芳族环; R 1和R 2独立地是氢，C 1-6烷基，芳基C 1-6烷基或与它们连接的氮原子一起形成任选地被取代的5-至7-元杂环，任选地含有另外的杂原子选自氮，硫或氧，氮原子被氢，C 1-6烷基，环C 3-7烷基或任选取代的芳基，杂芳基或芳基C 1-6烷基取代; R 3是氢或C 1-6烷基; X是氧，硫或键; n为2或3; m为1或2，具有药理活性，其制备方法，含有它们的组合物及其在治疗CNS疾病中的应用。

10. 发明申请

WO1997047602A1 TRICYCLIC AMINE DERIVATIVES 审中-公开
标题翻译：三元胺衍生物
公开(公告)号：WO1997047602A1
公开(公告)日：1997-12-18
申请号：PCT/EP1997002985
申请日：1997-06-06
申请人： SMITHKLINE BEECHAM PLC , STEMP, Geoffrey , JOHNSON, Christopher, Norbert , SMITH, Stephen, Allan , JEFFREY, Phillip
发明人： SMITHKLINE BEECHAM PLC
IPC分类号： C07D221/10
CPC分类号： C07D221/10 , C07D209/60
摘要： Compounds of formula (I) wherein R represents a group of formula (A) or (B); R represents a hydrogen atom or a C1-4alkyl group; R represents a substituent selected from: a hydrogen or halogen atom, a hydroxy, cyano, trifluoromethyl, trifluoromethoxy, trifluoromethanesulfonyloxy, C1-4alkyl, C1-4alkoxy, arylC1-4alkoxy, C1-4alkylthio, C1-4alkoxyC1-4alkyl, C3-6cycloalkylC1-4alkoxy, C1-4alkanoyl, C1-4alkoxycarbonyl, C1-4alkylsulphonyl, C1-4alkylsulphonyloxy, C1-4alkylsulphonylC1-4alkyl, arylsulphonyl, arylsulphonyloxy or arylsulphonylC1-4alkyl group, a group R OCO(CH2)p, R R NCO(CH2)p or R R NSO2(CH2)p where each of R and R independently represents a hydrogen atom or a C1-4alkyl group and p represents zero or an integer from 1 to 4, or a group Ar -Z, wherein Ar represents an optionally substituted phenyl ring or an optionally substituted 5- or 6-membered aromatic heterocyclic ring and Z represents a bond, O, S, or CH2; q is 1 or 2; T represents CH2, CH2CH2 or OCH2; V represents CH2, O or a bond; Ar and Ar each independently represent an optionally substituted phenyl ring or an optionally substituted 5- or 6-membered aromatic heterocyclic ring; and Y represents a bond, -NHCO-, -CONH-, -CH2-, or -(CH2)mY (CH2)n-, wherein Y represents O, S, SO2, or CO and m and n each represent zero or 1 such that the sum of m+n is zero or 1; and salts thereof have activity at dopamine receptors and are useful in the treatment of psychoses such as schizophrenia.
摘要翻译：式（I）的化合物，其中R 1表示式（A）或（B）的基团; R 2表示氢原子或C 1-4烷基; R 3表示选自：氢或卤素原子，羟基，氰基，三氟甲基，三氟甲氧基，三氟甲磺酰氧基，C 1-4烷基，C 1-4烷氧基，芳基C 1-4烷氧基，C 1-4烷硫基，C 1-4烷氧基C 1-4烷基，C 3 6-环烷基C 1-4烷氧基，C 1-4烷酰基，C 1-4烷氧基羰基，C 1-4烷基磺酰基，C 1-4烷基磺酰氧基，C 1-4烷基磺酰基C 1-4烷基，芳基磺酰基，芳基磺酰氧基或芳基磺酰基C 1-4烷基，R 3 OCO（CH 2）p， 3> R 4 NCO（CH 2）p或R 3 R 4 NSO 2（CH 2）p，其中R 3和R 4各自独立地表示氢原子或C 1-4烷基，p 表示0或1至4的整数，或Ar 2 -Z族，其中Ar 2表示任选取代的苯基环或任选取代的5或6元芳族杂环，Z表示键， O，S或CH2; q为1或2; T表示CH 2，CH 2 CH 2或OCH 2; V表示CH 2，O或键; Ar和Ar 1各自独立地表示任选取代的苯环或任选取代的5或6元芳族杂环; 并且Y表示键，-NHCO-，-CONH - ， - CH 2 - 或 - （CH 2）m Y 1（CH 2）n - ，其中Y 1表示O，S，SO 2或CO和m， n各自表示零或1，使得m + n的和为零或1; 其盐在多巴胺受体中具有活性，并且可用于治疗精神病如精神分裂症。

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