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1. 发明授权

US5541194A Certain 1-azabicyclo[2.2.1]heptanes and 1-azabicyclo[2.2.2]octanes 失效
标题翻译：某些1-氮杂双环[2.2.1]庚烷和1-氮杂双环[2.2.2]辛烷
公开(公告)号：US5541194A
公开(公告)日：1996-07-30
申请号：US369290
申请日：1995-01-06
申请人： Barry S. Orlek , Paul A. Wyman , Harry J. Wadsworth
发明人： Barry S. Orlek , Paul A. Wyman , Harry J. Wadsworth
IPC分类号： A61K31/395 , A61K31/435 , A61K31/55 , A61P25/02 , C07D453/02 , C07D471/08 , C07D487/08 , A61K31/44 , C07D221/02
CPC分类号： C07D487/08 , C07D453/02
摘要： Novel compounds of formula (I), processes for their preparation, and their use as pharmaceutical agents are described: ##STR1## in which p represents an integer of 2 to 4; r represents an integer of 1 or 2; s represents 0 or 1; and X represents a group ##STR2## in which A.sub.1 is oxygen or sulphur, one of A.sub.2 and A.sub.3 is CR.sub.1 and the other is nitrogen or CR.sub.2, or A.sub.2 is oxygen or sulphur, A.sub.1 is CH and A.sub.3 is CR.sub.1, where R.sub.1 and R.sub.2 are independently selected from hydrogen and C.sub.1-2 alkyl, with the proviso that when r is 2, R.sub.1 and R.sub.2 are hydrogen or methyl. The novel compounds of this invention may be used to treat or to prevent dementia in mammals.
摘要翻译：描述了新的式（I）化合物，其制备方法及其作为药剂的用途：其中p表示2至4的整数; r表示1或2的整数; s表示0或1; X表示A1为氧或硫的基团，其中A2和A3为CR1，另一个为氮或CR2，或A2为氧或硫，A1为CH，A3为CR1，其中R1和R2为独立地选自氢和C 1-2烷基，条件是当r为2时，R 1和R 2为氢或甲基。本发明的新化合物可用于治疗或预防哺乳动物的痴呆症。

2. 发明授权

US5521201A Method for treatment of atherosclerosis 失效
标题翻译：治疗动脉粥样硬化的方法
公开(公告)号：US5521201A
公开(公告)日：1996-05-28
申请号：US457387
申请日：1995-06-01
申请人： Richard M. Hindley , Michael A. Cawthorne
发明人： Richard M. Hindley , Michael A. Cawthorne
IPC分类号： A61K31/425 , A61K31/426 , A61K31/427 , C07D277/20 , C07D277/42 , C07D277/82 , C07D417/12 , A61K31/44
CPC分类号： A61K31/426 , A61K31/427 , C07D277/20 , C07D277/42 , C07D277/82 , C07D417/12
摘要： A method is provided for the treatment and/or prophylaxis of cardiovascular diseases in a human or non-human mammal, which comprises administering to a human or non-human mammal in need thereof, an effective, non-toxic amount of a compound of formula (I): ##STR1## or a tautomeric form thereof and/or a pharmaceuticlaly acceptable salt thereof and/or a pharmaceutically acceptable solvate thereof, in which A.sup.1 represents a substituted or unsubstituted aromatic heterocyclyl group; R.sup.1 represents a hydrogen atom, an alkyl group, an acyl group, an aralkyl group, wherein the aryl moiety may be substituted or unsubstituted, or a substituted or unsubstituted aryl group; R.sup.2 and R.sup.3 each represent hydrogen, or R.sup.2 and R.sup.3 together represent a bond; A.sup.2 represents a benzene ring having in total up to five substituents; and n represents an integer in the range of from 2 to 6.
摘要翻译：提供了用于治疗和/或预防人或非人哺乳动物心血管疾病的方法，其包括对有需要的人或非人哺乳动物施用有效的无毒量的式（I）化合物：其中A 1表示取代或未取代的芳族杂环基;（I）化合物或其互变异构形式和/或其药物可接受的盐和/或其药学上可接受的溶剂化物， R1表示氢原子，烷基，酰基，芳烷基，其中芳基部分可以是取代或未取代的，或取代或未取代的芳基; R2和R3各自表示氢，或R2和R3一起表示键; A2代表总共有五个取代基的苯环; n表示2〜6的整数。

3. 发明授权

US5371092A Use of paroxetine for the treatment of senile dementia, bulimia, migraine or anorexia 失效
标题翻译：使用帕罗西汀治疗老年痴呆症，贪食症，偏头痛或厌食症
公开(公告)号：US5371092A
公开(公告)日：1994-12-06
申请号：US64088
申请日：1993-05-21
申请人： Anthony M. Johnson
发明人： Anthony M. Johnson
IPC分类号： A61K31/4427 , A61K31/445 , A61P3/04 , A61P25/04 , A61P25/06 , A61P25/28 , C07D401/12 , A61K31/435
CPC分类号： A61K31/445
摘要： The method of using paroxetine or a pharmaceutically acceptable salt thereof for the treatment of senile dementia.
摘要翻译： PCT No.PCT / GB91 / 02062 Sec。 371日期：1993年5月21日 102（e）日期1993年5月21日PCT 1991年11月21日PCT PCT。第WO92 / 09281号公报日期：1992年6月11日。将帕罗西汀或其药学上可接受的盐用于治疗老年性痴呆的方法。

4. 发明授权

US5275816A Cephalosporin derivatives 失效
标题翻译：头孢菌素衍生物
公开(公告)号：US5275816A
公开(公告)日：1994-01-04
申请号：US578662
申请日：1990-09-04
申请人： Clive L. Branch , Angela W. Guest , Stephen C. Finch
发明人： Clive L. Branch , Angela W. Guest , Stephen C. Finch
IPC分类号： C07D463/00 , A61K31/445 , A61K31/535 , A61K31/545 , A61K31/546 , A61P31/04 , C07D501/00 , C07D501/57 , C07D505/00
CPC分类号： C07D501/00
摘要： 7 .alpha.-formamido cephalosporin derivatives having a 3[N-(optionally substituted)aminothiopyridinium thiomethyl] substituent have anti-bacterial activity and are of use in anti-bacterial therapy. Processes for the preparation thereof and intermediates for use in these processes are also disclosed.
摘要翻译：具有3（N-（任选取代的）氨基硫代吡啶硫基甲基）取代基的7（α） - 甲酰胺头孢菌素衍生物具有抗细菌活性并且在抗细菌治疗中有用。还公开了其制备方法和用于这些方法的中间体。

5. 发明授权

US5264436A Heterocyclic compounds which have useful pharmaceutical utility 失效
标题翻译：具有有用药物效用的杂环化合物
公开(公告)号：US5264436A
公开(公告)日：1993-11-23
申请号：US760405
申请日：1991-09-16
申请人： John M. Berge , Lee J. Beeley
发明人： John M. Berge , Lee J. Beeley
IPC分类号： C07D403/06 , A61K31/47 , C07D401/06
CPC分类号： C07D403/06
摘要： A compound of formula (I): ##STR1## or a pharmaceutically acceptable salt, ester or amide thereof, or a pharmaceutically acceptable solvate thereof, wherein:Z represents a residue of a substituted or unsubstituted aryl group,A.sub.1 represents a substituted or unsubstituted methylene group or a substituted or unsubstituted ethylene group;A.sub.2 represents a substituted or unsubstituted methylene group or a substituted or unsubstituted ethylene group;providing that at least one of A.sup.1 or A.sup.2 represents a substituted methylene group or a substituted ethylene group,X represents O or NR.sup.o wherein R.sup.o represents a hydrogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, an alkanoyl group substituted or unsubstituted in the alkyl moiety, or an arylalkyl moiety substituted or unsubstituted in the aryl moiety,p represents an integer 2 or 3, andq represents an integer in the range of from 1 to 12;a process for preparing such a compound, a composition comprising such a compound and the use of such a compound in medicine.
摘要翻译：式（I）化合物：其中：Z表示取代或未取代的芳基的残基，A1表示取代或未取代的芳基，或未取代的亚甲基或取代或未取代的亚乙基; A2表示取代或未取代的亚甲基或取代或未取代的亚乙基; 条件是A1或A2中的至少一个表示取代的亚甲基或取代的亚乙基，X表示O或NRo，其中Ro表示氢原子，取代或未取代的烷基，取代或未取代的芳基，取代的烷酰基或在烷基部分未取代，或在芳基部分取代或未取代的芳烷基部分，p表示2或3的整数，q表示1至12的整数; 制备这种化合物的方法，包含这种化合物的组合物和这种化合物在医药中的用途。

6. 发明授权

US5254557A Compound and treatment 失效
标题翻译：复方和治疗
公开(公告)号：US5254557A
公开(公告)日：1993-10-19
申请号：US892619
申请日：1992-06-01
申请人： Derek R. Buckle , David G. Smith , Frederick Cassidy
发明人： Derek R. Buckle , David G. Smith , Frederick Cassidy
IPC分类号： A61K31/435 , C07D405/04 , C07D491/04 , C07D491/052 , C07D401/14 , A61K31/44 , A61K31/505 , C07D403/14
CPC分类号： C07D405/04 , A61K31/435 , C07D491/04
摘要： A compound of formula (IA) in the form of a pharmaceutically acceptable microfine powder is disclosed. ##STR1##
摘要翻译：公开了药学上可接受的超细粉末形式的式（IA）化合物。（图）

7. 发明授权

US5252575A Antiviral purine derivatives with improved gastrointestinal absorption 失效
标题翻译：具有改善胃肠道吸收的抗病毒嘌呤衍生物
公开(公告)号：US5252575A
公开(公告)日：1993-10-12
申请号：US886710
申请日：1992-05-21
申请人： Michael R. Harnden , Paul G. Wyatt , Leslie J. A. Jennings
发明人： Michael R. Harnden , Paul G. Wyatt , Leslie J. A. Jennings
IPC分类号： C07D473/18 , C07D473/32 , A61K31/52 , C07D473/26
CPC分类号： C07D473/32 , C07D473/18
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is hydrogen or hydroxy; andR.sub.2 is C.sub.1-6 alkyl;which are pro-drugs for 9-(3-hydroxyprop-1-oxy)guanine having antiviral activity, a process for their preparation and their use as pharmaceuticals.
摘要翻译：式（I）化合物及其药学上可接受的盐：其中R 1是氢或羟基; 和R 2是C 1-6烷基; 其为具有抗病毒活性的9-（3-羟基丙-1-氧）鸟嘌呤的前药，其制备方法及其作为药物的用途。

8. 发明授权

US5232938A Certain 1,2,4-triazole(oxy or amino)benzopyran derivatives having pharmacological activity 失效
标题翻译：某些具有药理活性的1,2,4-三唑（氧基或氨基）苯并吡喃衍生物
公开(公告)号：US5232938A
公开(公告)日：1993-08-03
申请号：US873587
申请日：1992-04-21
申请人： Geoffrey Stemp , Gordon Burrell
发明人： Geoffrey Stemp , Gordon Burrell
IPC分类号： C07D249/12 , C07D249/14 , C07D401/12 , C07D405/12 , C07D491/04 , C07F9/6518 , C07F9/6558
CPC分类号： C07D401/12 , C07D249/12 , C07D249/14 , C07D405/12 , C07D491/04 , C07F9/65182 , C07F9/65187 , C07F9/65586
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein a, b, J, Y and R.sub.2 -R.sub.8 are as defined herein are potassium channel activators, a process for their preparation and their pharmaceutical use.
摘要翻译：式（I）化合物及其药学上可接受的盐：其中a，b，J，Y和R 2 -R 8如本文所定义的是钾通道活化剂，其制备方法及其药物用途。

9. 发明授权

US5200413A Indolyl carboxamides useful treating migraine, cluster headache, trigeminal neuralgia or emesis 失效
标题翻译：吲哚甲酰胺可用于治疗偏头痛，丛集性头痛，三叉神经痛或呕吐
公开(公告)号：US5200413A
公开(公告)日：1993-04-06
申请号：US740397
申请日：1991-08-05
申请人： Francis D. King , Karen A. Joiner
发明人： Francis D. King , Karen A. Joiner
IPC分类号： C07D451/04
CPC分类号： C07D451/04
摘要： Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein L is NH;X and Y are independently selected from hydrogen or C.sub.1-4 alkyl, or together are a bond;R.sub.1 and R.sub.2 are independently selected from hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl-C.sub.1-4 alkyl, or together are C.sub.2-4 polymethylene;R.sub.3 and R.sub.4 are independently selected from hydrogen, halogen, CF.sub.3, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.1-7 acyl, C.sub.1-7 acylamino, C.sub.1-6 alkylsulphonylamino, N-(C.sub.1-6 alkylsulphonyl)-N-C.sub.1-4 alkylamino, C.sub.1-6 alkylsulphinyl, hydroxy, nitro or amino, aminocarbonyl, aminosulphonyl, aminosulphonylamino or N-(aminosulphonyl)-C.sub.1-4 alkylamino optionally N-substituted by one or two groups selected from C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl C.sub.1-4 alkyl, phenyl or phenyl C.sub.1-4 alkyl groups or optionally N-disubstituted by C.sub.4-5 polymethylene;Z is a group of formula (a) ##STR2## wherein n is 2 or 3;p is 1 or 2;q is 1 to 3;r is 1 to 3; andR.sub.5 or R.sub.6 is C.sub.1-7 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkyl-C.sub.1-2 alkyl or C.sub.2-7 alkenyl-C.sub.1-4 alkyl;having 5-HT M-receptor antagonist activity.
摘要翻译：式（I）化合物及其药学上可接受的盐：其中L是NH; X和Y独立地选自氢或C 1-4烷基，或一起是一个键; R 1和R 2独立地选自氢，C 1-6烷基，C 2-6烯基-C 1-4烷基，或一起是C 2-4亚甲基; R 3和R 4独立地选自氢，卤素，CF 3，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基，C 1-7酰基，C 1-7酰氨基，C 1-6烷基磺酰基氨基，N-（C 1-6烷基磺酰基）-N-C 1-4烷基氨基，C 1-6烷基亚磺酰基，羟基，硝基或氨基，氨基羰基，氨基磺酰基，氨基磺酰基氨基或N-（氨基磺酰基）-C 1-4烷基氨基，其任选地被一个或两个选自C 1-6 烷基，C 3-8环烷基，C 3-8环烷基C 1-4烷基，苯基或苯基C 1-4烷基或任选被C 4-5多亚甲基N-二取代; Z是式（a）的基团，其中n为2或3; p为1或2; q为1〜3; r为1〜3; 且R 5或R 6为C 1-7烷基，C 3-8环烷基，C 3-8环烷基-C 1-2烷基或C 2-7烯基-C 1-4烷基; 具有5-HT M受体拮抗剂活性。

10. 发明授权

US5190937A Lactam derivatives 失效
标题翻译： LACTAM衍生物
公开(公告)号：US5190937A
公开(公告)日：1993-03-02
申请号：US640069
申请日：1991-01-11
申请人： Roger E. Markwell , Ian Hughes
发明人： Roger E. Markwell , Ian Hughes
IPC分类号： A61K31/395 , A61P29/00 , A61P43/00 , C07D223/12 , C07D225/02 , C12N9/99
CPC分类号： C07D223/12 , C07D225/02
摘要： Novel compounds of formula (I), and pharmaceutically acceptable salts thereof; their preparation; compositions containing them; and their use in the treatment of conditions in which degradation of connective tissue and other proteinaceous components of the body occurs: ##STR1## in which, R.sub.1 is --OH; alkoxy; aryloxy or aralkyloxy in each of which the aryl group is optionally substituted; --NR.sub.6 R.sub.7, where each of R.sub.6 and R.sub.7 is independently hydrogen or alkyl, or R.sub.6 and R.sub.7 together with the nitrogen atom to which they are bonded form a 5-, 6- or 7-membered ring with an optional oxygen or sulphur atom or an optionally substituted second nitrogen atom in the ring; or a group:--NH--CH(R.sub.8)--C(O)--R.sub.9where R.sub.8 is hydrogen; alkyl optionally substituted by --OH, alkoxy, --NR.sub.6 R.sub.7 as defined for R.sub.1, guanidine, --CO.sub.2 H, --CONH.sub.2, --SH, or --S--alkyl; or --CH.sub.2 --Ar where Ar is optionally substituted aryl or heteroaryl; and R.sub.9 is alkoxy; --OH; or --NR.sub.6 R.sub.7 as defined for R.sub.1 ; R.sub.2 is hydrogen; C.sub.2-8 alkanoyl; or optionally substituted aroyl; R.sub.3 is C.sub.3-6 alkyl; and R.sub.4 is --(CH.sub.2).sub.m -- where m is an integer from 4 to 12.

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