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1. 发明授权

US4663320A (2-oxo-1,2,3,5-tetrahydroimidazo[2,1-b]quinoazolinyl)oxyalkylamides, compositions and the use thereof 失效
公开(公告)号：US4663320A
公开(公告)日：1987-05-05
申请号：US744100
申请日：1985-06-11
申请人： Gordon H. Jones , Michael C. Venuti , Robert Alvarez , John J. Bruno , Jurg R. Pfister
发明人： Gordon H. Jones , Michael C. Venuti , Robert Alvarez , John J. Bruno , Jurg R. Pfister
IPC分类号： C07C205/37 , C07C205/44 , C07C205/56 , C07D209/08 , C07D215/08 , C07D217/06 , C07D295/185 , C07D487/04 , A61K31/55 , A61K31/505 , C07D213/08 , C07D213/14
CPC分类号： C07D295/185 , C07C205/37 , C07C205/44 , C07C205/56 , C07D209/08 , C07D215/08 , C07D217/06 , C07D487/04
摘要： Compounds according to the formula ##STR1## an optical isomer thereof, or a pharmaceutically acceptable acid addition salt thereof wherein:n is an integer of 1 to 6;R.sub.1 is hydrogen or alkyl of 1 to 4 carbons;R.sub.2 is hydrogen or R.sub.1 and R.sub.2 are combined to form an oxo group;R.sub.3 is hydrogen, alkyl of 1 to 6 carbons, phenyl, benzyl, hydroxy lower alkyl or an aliphatic acylate thereof of 1 to 6 carbon atoms or an aryl acylate thereof of 7 to 12 carbon atoms, carbamoyl alkyl, carboxyalkyl, alkoxycarbonylalkyl of an .alpha.-amino acid side chain;R.sub.4 is hydrogen, alkyl of 1 to 6 carbons, benzyl, or hydroxy lower alkyl;Y is hydrogen, alkyl of 1 to 4 carbon atoms, halo or lower alkoxy;A is NR.sub.5 R.sub.6 wherein R.sub.5 and R.sub.6 are independently selected from the group consisting of: hydrogen; alkyl of 1 to 6 carbon atoms; hydroxyalkyl of 1 to 6 carbon atoms or an aliphatic acylate thereof of 1 to 6 carbon atoms or an aryl acrylate thereof of 7 to 12 carbon atoms; cycloalkyl of 3 to 8 carbon atoms or cycloalkyl lower alkyl of 4 to 12 carbon atoms wherein the cycloalkyl ring is unsubstituted or substituted with a lower alkyl, lower alkoxy, --OH, --OCOR.sub.7, halo, --NH.sub.2, --N(R.sub.7).sub.2, --NHCOR.sub.7, --COOH, or --COO(R.sub.7) group wherein R.sub.5 is lower alkyl; and phenyl or phenyl lower alkyl wherein phenyl is unsubstituted or substituted with at least one lower alkyl, halo or lower alkoxy group or an --NH.sub.2, --N(R.sub.7).sub.2, --NHCOR.sub.7, --COOH, or --COOR.sub.7 group wherein R.sub.7 is lower alkyl; or wherein R.sub.5 and R.sub.6 are combined to form a compound selected from the group consisting of: morpholinyl; piperidinyl; perhexylenyl; N-loweralkylpiperazinyl; pyrrolidinyl; tetrahydroquinolinyl; tetrahydroisoquinolinyl; (.+-.)-decahydroquinolinyl and indolinyl. These compounds are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic agents and the like in mammals. The compounds also have inotropic and anti-metastatic activities.

2. 发明授权

US06958355B2 Materials and methods for the treatment of diabetes, hyperlipidemia, hypercholesterolemia, and atherosclerosis 失效
公开(公告)号：US06958355B2
公开(公告)日：2005-10-25
申请号：US10251522
申请日：2002-09-20
申请人： Pascal Druzgala , Peter G. Milner , Jurg R. Pfister
发明人： Pascal Druzgala , Peter G. Milner , Jurg R. Pfister
IPC分类号： A61P3/10 , C07D261/12 , C07D277/20 , C07D277/34 , C07D311/70 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07J3/00 , A61K31/421 , C07D263/58
CPC分类号： C07D277/20 , C07D261/12 , C07D277/34 , C07D311/70 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07J3/00 , Y10S514/866
摘要： The subject invention provides pharmaceutical compounds useful in the treatment of Type II diabetes. These compounds are advantageous because they are readily metabolized by the metabolic drug detoxification systems. Particularly, thiazolidinedione analogs that have been designed to include esters within the structure of the compounds are provided. This invention is also drawn to methods of treating disorders, such as diabetes, comprising the administration of therapeutically effective compositions comprising compounds that have been designed to be metabolized by serum or intracellular hydrolases and esterases. Pharmaceutical compositions of the ester-containing thiazolidinedione analogs are also taught.

3. 发明授权

US5789416A N.sup.6 mono heterocyclic substituted adenosine derivatives 失效
标题翻译： N6单杂环取代的腺苷衍生物
公开(公告)号：US5789416A
公开(公告)日：1998-08-04
申请号：US702234
申请日：1996-08-27
申请人： Robert T. Lum , Jurg R. Pfister , Steven R. Schow , Michael M. Wick , Marek G. Nelson , George F. Schreiner
发明人： Robert T. Lum , Jurg R. Pfister , Steven R. Schow , Michael M. Wick , Marek G. Nelson , George F. Schreiner
IPC分类号： C07H19/167 , A61K31/00 , A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/706 , A61K31/7064 , A61K31/7076 , A61P5/24 , A61P9/00 , A61P9/06 , A61P43/00 , C07D20060101 , C07H19/16 , C07D487/04
CPC分类号： C07H19/16
摘要： A substituted N.sup.6 -oxa, thia, thioxa and azacycloalkyl substituted adenosine derivative and a method for using the composition as an A.sub.1 heart adenosine receptor.
摘要翻译：取代的N6-氧杂，硫杂，硫杂和氮杂环烷基取代的腺苷衍生物和使用该组合物作为A1心脏腺苷受体的方法。

4. 发明授权

US4543361A .+-.2-[Phenethyl]-5-[(3,4-methylenedioxy)-.alpha.-hydroxybenzyl]py rrolidine antihypertensives and use thereas 失效
标题翻译： +/- 2- [苯乙基] -5 - [（3,4-亚甲二氧基）-α-羟基苄基]吡咯烷抗高血压药物，并在其中使用
公开(公告)号：US4543361A
公开(公告)日：1985-09-24
申请号：US527717
申请日：1983-08-29
申请人： Joseph M. Muchowski , Robert Greenhouse , Jack Ackrell , Tsung-Tee Li , Jurg R. Pfister
发明人： Joseph M. Muchowski , Robert Greenhouse , Jack Ackrell , Tsung-Tee Li , Jurg R. Pfister
IPC分类号： C07D295/108 , C07D317/60 , C07D405/06 , A61K31/40 , C07D405/02
CPC分类号： C07D295/108 , C07D317/60 , C07D405/06
摘要： A compound of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof are potent antihypertensive agents and are therefore useful as cardiovascular system regulators.
摘要翻译：式“IMAGE”及其药学上可接受的酸加成盐的化合物是有效的抗高血压药，因此可用作心血管系统调节剂。

5. 发明授权

US4353922A Anticholinergic bronchodilators 失效
标题翻译：抗胆碱能支气管扩张剂
公开(公告)号：US4353922A
公开(公告)日：1982-10-12
申请号：US243674
申请日：1981-03-13
申请人： Jurg R. Pfister
发明人： Jurg R. Pfister
IPC分类号： C07D303/36 , C07D487/08 , A61K31/40
CPC分类号： C07D487/08 , C07D303/36 , Y10S514/826
摘要： Compounds of the formula ##STR1## wherein the serrated lines denote both endo and exo forms; R.sub.1 and R.sub.2 are the same or different and are C.sub.1 to C.sub.6 alkyl, C.sub.5 or C.sub.6 cycloalkyl, C.sub.5 or C.sub.6 cycloalkenyl, phenyl optionally substituted with C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy or halo, or 5 or 6 membered heterocyclic aryl wherein the heteroatom is oxygen, nitrogen or sulfur; R.sub.3 is a C.sub.1 to C.sub.6 alkyl radical; R.sub.4 and X are optionally present, and when present R.sub.4 is a C.sub.1 to C.sub.6 alkyl radical or hydrogen and X is an inorganic or organic anion which forms a pharmaceutically acceptable salt. Methods for preparing these compounds are also disclosed. The compounds of the present invention are useful as anticholinergic agents.
摘要翻译：式“IMAGE”的化合物，其中锯齿状线表示内部和外部形式; R1和R2相同或不同，为C1至C6烷基，C5或C6环烷基，C5或C6环烯基，任选被C1至C6烷基取代的苯基，C1至C6烷氧基或卤素，或5或6元杂环芳基，其中杂原子是氧，氮或硫; R3是C1-C6烷基; R4和X任选存在，当存在时R4是C1-C6烷基或氢，X是形成药学上可接受的盐的无机或有机阴离子。还公开了制备这些化合物的方法。本发明的化合物可用作抗胆碱剂。

6. 发明授权

US4217361A Disubstituted xanthone-2-carboxylic acid antiallergy agents 失效
标题翻译：二取代的呫吨酮-2-羧酸抗过敏剂
公开(公告)号：US4217361A
公开(公告)日：1980-08-12
申请号：US908312
申请日：1978-05-22
申请人： Jurg R. Pfister
发明人： Jurg R. Pfister
IPC分类号： C07D311/86 , A61K31/35
CPC分类号： C07D311/86
摘要： Compositions containing and methods employing, as the essential ingredient, novel substituted xanthone-2-carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed.
摘要翻译：含有可用于治疗过敏症状的新型取代的呫吨酮-2-羧酸化合物作为必需成分的组合物和方法。还公开了制备这些化合物及其组合物和中间体的方法。

7. 发明授权

US3951618A Method of use of, and compositions containing, disubstituted xanthone carboxylic acid compounds 失效
标题翻译：使用方法和含有二取代的呫吨酮羧酸化合物的组合物
公开(公告)号：US3951618A
公开(公告)日：1976-04-20
申请号：US542477
申请日：1975-01-20
申请人： Jurg R. Pfister , Ian T. Harrison , John H. Fried
发明人： Jurg R. Pfister , Ian T. Harrison , John H. Fried
IPC分类号： C07D311/86 , A61K31/35
CPC分类号： C07D311/86
摘要： Compositions containing and methods employing, as the essential ingredient, novel disubstituted xanthone carboxylic acid compounds which are useful in the treatment of allergic conditions. Methods for preparing these compounds and compositions and intermediates therein are also disclosed. 5-Methylthio-7-isopropoxyxanthone-2-carboxylic acid and 5,7-di-(methylthio)xanthone-2-carboxylic acid are illustrated as representative compounds.
摘要翻译：含有可用于治疗过敏症状的新型二取代呫吨酮羧酸化合物作为必需成分的组合物和方法。还公开了制备这些化合物及其组合物和中间体的方法。 5-甲硫基-7-异丙氧基呫吨酮-2-羧酸和5,7-二（甲硫基）呫吨酮-2-羧酸作为代表性化合物。

8. 发明申请

US20090088418A1 4-SUBSTITUTED QUINUCLIDINE DERIVATIVES, METHODS OF PRODUCTION, AND PHARMACEUTICAL USES THEREOF 有权
标题翻译： 4-取代的喹啉衍生物，生产方法及其药物用途
公开(公告)号：US20090088418A1
公开(公告)日：2009-04-02
申请号：US12242389
申请日：2008-09-30
申请人： Jurg R. Pfister , Meenakshi S. Venkatraman , Xiaoming Zhang
发明人： Jurg R. Pfister , Meenakshi S. Venkatraman , Xiaoming Zhang
IPC分类号： A61K31/55 , C07D453/02 , A61K31/439 , A61K31/407 , C07D487/04
CPC分类号： C07D453/02 , C07D471/08
摘要： The present invention relates to compounds and formulations capable of affecting nicotinic acetylcholine receptors (nAChRs), for example, as modulators of specific nicotinic receptor subtypes (specifically, the alpha7 nAChR subtype). The present invention also relates to methods for treating a wide variety of conditions and disorders, particularly those associated with dysfunction of the central and autonomic nervous systems.
摘要翻译：本发明涉及能够影响烟碱乙酰胆碱受体（nAChR）的化合物和制剂，例如作为特异性烟碱受体亚型（特别是α7nAChR亚型）的调节剂。本发明还涉及用于治疗各种各样的病症和疾病的方法，特别是与中枢神经系统和自主神经系统的功能障碍有关的方法。

9. 发明申请

US20080132561A1 Materials and Methods for Treating Hypercholesterolemia 审中-公开
标题翻译：治疗高胆固醇血症的材料与方法
公开(公告)号：US20080132561A1
公开(公告)日：2008-06-05
申请号：US12027552
申请日：2008-02-07
申请人： Pascal Druzgala , Xiaoming Zhang , Jurg R. Pfister
发明人： Pascal Druzgala , Xiaoming Zhang , Jurg R. Pfister
IPC分类号： A61K31/405 , A61P9/00
CPC分类号： C07D239/42 , A61K31/405 , A61K31/47 , A61K31/505 , C07C69/675 , C07C69/708 , C07C69/732 , C07C2602/28 , C07D207/34 , C07D209/12 , C07D209/24 , C07D213/55 , C07D215/14 , C07D307/80 , C07D311/72
摘要： The subject invention provides novel HMG-CoA-reductase inhibitors. In a preferred embodiment, the HMG-CoA reductase inhibitors of the subject invention can be deactivated to a primary inactive metabolite by hydrolytic enzymes. Compounds of the present invention can be advantageously used to treat patients suffering hypercholesterolemia.
摘要翻译：本发明提供新的HMG-CoA还原酶抑制剂。在优选的实施方案中，本发明的HMG-CoA还原酶抑制剂可以通过水解酶而失活至初级无活性代谢物。本发明的化合物可有利地用于治疗患有高胆固醇血症的患者。

10. 发明授权

US5889007A 10, 11-methanodibenzosuberane derivatives 失效
标题翻译： 10,11-甲烷二苯并三唑衍生物
公开(公告)号：US5889007A
公开(公告)日：1999-03-30
申请号：US436992
申请日：1995-05-08
申请人： Jurg R. Pfister , Doris L. Slate
发明人： Jurg R. Pfister , Doris L. Slate
IPC分类号： C07D295/08 , A61K31/495 , A61P33/02 , A61P35/00 , C07D213/65 , C07D215/20 , C07D215/26 , C07D271/12 , C07D295/092 , C07D401/12 , C07D413/12 , A61K31/50
CPC分类号： C07D295/088 , C07D213/65 , C07D215/20 , C07D215/26 , C07C2103/40
摘要： 10,11-Methanodibenzosuberane derivatives, i.e., the compounds of Formula I: ##STR1## wherein: A is --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHR.sup.a --CH.sub.2 --, or --CH.sub.2 --CHR.sup.a --CHR.sup.b --CH.sub.2 --, where one of R.sup.a or R.sup.b is H, OH, or lower acyloxy, and the other is H;R.sup.1 is H, P, Cl or Br;R.sup.2 is H, F, Cl or Br; andR.sup.3 is heteroaryl or phenyl optionally substuted with F, Cl, Br, CF.sub.3, CN, NO.sub.2 or OCHF.sub.2 ;and the pharmaceutically acceptable salts thereof, are useful chemosensitizing agents, e.g., for cancer chemotherapy, particularly for treating multidrug resistance.
摘要翻译： 10,11-甲烷二苯并环烷衍生物，即式I的化合物：其中：A是-CH 2 -CH 2 - ， - CH 2 -CHR a -CH 2 - 或-CH 2 -CHR a -CHR b -CH 2 - ，其中 Ra或Rb之一是H，OH或低级酰氧基，另一个是H; R1是H，P，Cl或Br; R2是H，F，Cl或Br; 并且R 3是杂芳基或任选被F，Cl，Br，CF 3，CN，NO 2或OCHF 2取代的苯基; 和其药学上可接受的盐是有用的化学敏化剂，例如用于癌症化疗，特别是用于治疗多药耐药性。

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