| 序号 | 专利名 | 申请号 | 申请日 | 公开（公告）号 | 公开（公告）日 | 发明人 |
|---|---|---|---|---|---|---|
| 1 | 作为AMPA受体正性调节剂的（噻吩并）-[f]-氧杂吖庚因-5-酮衍生物 | CN200610059885.8 | 2002-06-10 | CN101029051B | 2010-06-09 | S·J·A·格罗夫; J·亚当-沃勒尔; 张明强; R·吉尔福兰 |
| 本发明涉及具有通式(I)的(吡啶并/噻吩并)-[f]-氧杂吖庚因-5-酮衍生物或其药学上可接受的盐，其中R1、R2和R3独立地为H或(C1-4)烷基；Ar代表稠合的噻吩或吡啶环，所述基团任选被一个或多个选自以下的取代基取代：(C1-4)烷基、(C1-4)烷氧基、(C1-4)烷氧基(C1-4)烷基、CF3、卤素、硝基、氰基、NR4R5、NR4COR6和CONR4R5；R4和R5独立地为H或(C1-4)烷基；或者R4和R5与它们结合的氮原子一起形成5-或6-元饱和杂环，所述杂环任选包含其它选自O、S或NR6的杂原子；R6为(C1-4)烷基；A代表4-7元饱和杂环的残基，任选包含氧原子，所述的环任选被1-3个选自以下的取代基取代：(C1-4)烷基、(C1-4)烷氧基、羟基、卤素和氧。本发明还涉及包含所述衍生物的药物组合物以及这些(吡啶并/噻吩并)-[f]-氧杂吖庚因-5-酮衍生物在对中枢神经系统中的AMPA受体介导的突触反应的增强有应答的神经病和精神病的治疗中的应用。 | ||||||
| 2 | 作为AMPA受体正性调节剂的（噻吩并）－[f]－氧杂吖庚因－5－酮衍生物 | CN200610059885.8 | 2002-06-10 | CN101029051A | 2007-09-05 | S·J·A·格罗夫; J·亚当-沃勒尔; 张明强; R·吉尔福兰 |
| 本发明涉及具有通式(I)的(吡啶并/噻吩并)－[f]－氧杂吖庚因－5－酮衍生物或其药学上可接受的盐，其中R1、R2和R3独立地为H或(C1－4)烷基；Ar代表稠合的噻吩或吡啶环，所述基团任选被一个或多个选自以下的取代基取代：(C1－4)烷基、(C1－4)烷氧基、(C1－4)烷氧基(C1－4)烷基、CF3、卤素、硝基、氰基、NR4R5、NR4COR6和CONR4R5；R4和R5独立地为H或(C1－4)烷基；或者R4和R5与它们结合的氮原子一起形成5－或6－元饱和杂环，所述杂环任选包含其它选自O、S或NR6的杂原子；R6为(C1－4)烷基；A代表4－7元饱和杂环的残基，任选包含氧原子，所述的环任选被1－3个选自以下的取代基取代：(C1－4)烷基、(C1－4)烷氧基、羟基、卤素和氧。本发明还涉及包含所述衍生物的药物组合物以及这些(吡啶并/噻吩并)－[f]－氧杂吖庚因－5－酮衍生物在对中枢神经系统中的AMPA受体介导的突触反应的增强有应答的神经病和精神病的治疗中的应用。 | ||||||
| 3 | Replacement thia cycloalkenyl Roh [3,2-b] pyridine | JP8591687 | 1987-04-09 | JP2561269B2 | 1996-12-04 | CHAARUZU EFU SHUENDAA; JON EICHI DOTSUDO |
| 4 | Novel azetidinone derivative and salt thereof | JP12917184 | 1984-06-25 | JPS6110581A | 1986-01-18 | YOSHIDA CHIYOUSAKU; TANAKA KIYOSHI; OCHIAI YUUICHI; NAKANO JIYOUJI; FUKUOKA |
| NEW MATERIAL:A compound expressed by formula I (R 1 is H, lower alkyl, halogeno-lower alkyl, etc.; R 2 is amino which may be protected; R 3 is halogen, amino and hydroxyl which may be protected etc.; R 4 is tetrazolyl; the wavy line part is syn or anti isomer or a mixture thereof). EXAMPLE: ( 3S,4R )-3-[2-( 2-Aminothiazol-4-yl )-(Z)-2-[( pyridin-3-yl) methoxyimino] acetamido]-4-methyl-1-(1H)-tetrazol-5-yl)-2-azetidinone. USE: An antimicrobial agent exhibiting improved activity against Gram-positive and Gram-negative bacteria. PREPARATION: A compound expressed by formula II is acylated with a compound expressed by formula III in or in the absence of a solvent at -50W+80°C to give the aimed compound expressed by formula I. The reaction can be carried out in the presence of a base, e.g. NaOH or triethylamine. COPYRIGHT: (C)1986,JPO&Japio | ||||||
| 5 | Short half-life-tetrazol containing rapamycin analog | JP2000512835 | 1998-09-24 | JP3790424B2 | 2006-06-28 | モリソン，カール・ダブリユ |
| 6 | Novel azetidinone derivatives and salts thereof | JP12917184 | 1984-06-25 | JPH075592B2 | 1995-01-25 | 譲二 中野; 長作 吉田; 勇 才川; 賢 田井; 清 田仲; 義和 福岡; 裕一 落合 |
| 7 | Substituted thiacycloalkeno(3,2-b)pyridines | JP8591687 | 1987-04-09 | JPS62289582A | 1987-12-16 | CHIYAARUZU EFU SHIYUUENDAA; JIYON EICHI DOTSUDO |
| 8 | JPS62187453A - | JP28095386 | 1986-11-27 | JPS62187453A | 1987-08-15 | |
| 9 | Short half-life-tetrazol containing rapamycin analog | JP2000512835 | 1998-09-24 | JP2001517671A | 2001-10-09 | モリソン，カール・ダブリユ |
| (57)【要約】 【課題】 望ましい免疫調節活性を持ちながらも、半減期が短縮されることにより不要な副作用を最小限に抑えられた免疫抑制剤を提供すること。 【解決手段】 式（Ｉ）を有する化合物、あるいはその薬学上許容し得る塩またはプロドラッグは、免疫調節剤であり、再狭窄および免疫若しくは自己免疫疾患の治療において有用である。 また、半減期を短縮して副作用を最小限に抑えた、癌阻害、真菌増殖阻害、再狭窄阻害、移植後組織拒絶反応阻害、および免疫若しくは自己免疫疾患阻害組成物、ならびに、癌、真菌増殖、再狭窄、移植後組織拒絶反応、および免疫若しくは自己免疫疾患の阻害方法も開示されている。 【化１】 | ||||||
| 10 | Thioether compounds used in the preparation of the bifunctional chelating agents for radioactive pharmaceutical for treatment | JP52832995 | 1995-04-25 | JPH09512796A | 1997-12-22 | メーラ ヴェンカテス; ウィン エイ ヴォルカート; アレン アール ケートリング; シルヴィア ジュリッソン; エルマー シュレンパー |
| (57)【要約】 治療用の 105 Rh-放射性製薬の調製に使用するための、十分に高い比放射能の 105 Rhと錯体を形成するために２個以上のチオエーテル基を含む多座配位子から本質的になる化合物。 | ||||||
| 11 | Suppressing methods and compositions of the 5α- reductase activity | JP50328694 | 1993-04-30 | JPH08501771A | 1996-02-27 | リャオ，シューツン; リャン，テーミン |
| (57)【要約】 本明細書において、飽和および不飽和脂肪酸類、その誘導体と合成類縁物質を含む新規クラスの抗アンドロゲン化合物類、その合成方法、およびアンドロゲン活性に起因する疾患の治療へのこれらの化合物の使用を開示する。 さらにまた、抗アンドロゲン活性があることがこれまで分からなかった公知の化合物の、アンドロゲン活性に起因する疾患の治療における使用も開示する。 | ||||||
| 12 | Novel dihydropyridine | JP18999885 | 1985-08-30 | JPS6165867A | 1986-04-04 | ANDORUU JIYON GIRUBII BAKUSUTA; KENESU JIYON GUURUDO; JIYON DEIKUSON; ARAN CHIYAARUZU TEINKAA |
| 13 | Monomers, polymers and photoresist compositions | US15858129 | 2017-12-29 | US11487203B2 | 2022-11-01 | Eui Hyun Ryu; Myung-Yeol Kim; Woo-Hyung Lee; Haemi Jeong; Kwang-Hwyi Im |
| Monomers and polymers are provided that comprise a carbon alicyclic group or heteroalicyclic group that comprises 1) one or more acid-labile ring substituents and 2) one or more ether or thioether ring substituents. Photoresists that comprise such polymers also are provided. | ||||||
| 14 | Polar nematic compounds | US13456727 | 2012-04-26 | US08709280B2 | 2014-04-29 | Bryan Ringstrand; Piotr Kaszynski |
| Polar nematic compounds having the following structure: where is a caged boron structure. The sphere of the caged boron structure is C and each non-sphere vertex of the caged boron structure is B—H. R is H, an alkyl, a cycloalkyl, a bicycloalkyl, an alkenyl, a cycloalkenyl, a bicycloalkenyl, an alkynyl, an acyl, an aryl, an alkylaryl, a halogen, a cyano group, an isothiocyanoto group, or a group that forms an ether, a ketone, an ester, a thioester, a sulfide, or a sulfone. R′ is H, an alkyl, a cycloalkyl, a bicycloalkyl, an alkenyl, a cycloalkenyl, a bicycloalkenyl, an alkynyl, an aryl, an alkylaryl, or a halogen. The compounds may be used in liquid crystal displays, and in television sets, laptop computers, computer monitors, hand-held communication devices, gaming devices, watches, cash registers, clocks, and calculators having liquid crystal displays. | ||||||
| 15 | Process for preparing an alpha-lipoic acid/cyclodextrin complex and product prepared | US11302810 | 2005-12-14 | US07737269B2 | 2010-06-15 | Helmut Reuscher; Mark Bauer |
| The invention relates to a process for the preparation of a cyclodextrin/alpha-lipoic acid complex, wherein in a first step, an alpha-lipoic acid and a cyclodextrin are dissolved in an aqueous alkaline solution having a pH above pH 7, and in a second step an acid is added to lower the pH of the solution to a pH below pH 7. | ||||||
| 16 | Methods and compositions for inhibiting 5.alpha.-reductase activity | US904443 | 1992-07-01 | US5422371A | 1995-06-06 | Shutsung Liao; Tehming Liang |
| Disclosed are a novel class of anti-androgenic compounds including saturated and unsaturated fatty acids, their derivatives, and synthetic analogs, according to the following formula:CH.sub.3 --(CH.sub.2).sub.a --(CR.sub.1 R.sub.2 CH.dbd.CH).sub.b --(CH.sub.2).sub.c --COOH,wherein R.sub.1 and R.sub.2 are each either hydrogen or a halogen; wherein a and c are integers from 0-9; wherein b is an integer from 1-6, provided that12<a+c+(3.times.b).ltoreq.22.Also disclose are methods of synthesis of these compounds, and their use in treating disorders associated with androgenic activities. Also disclosed is the use of known compounds not previously known for their anti-androgenic activity in treating disorders related to androgenic activities. | ||||||
| 17 | THIOETHER COMPOUNDS FOR USE IN PREPARING BIFUNCTIONAL CHELATING AGENTS FOR THERAPEUTIC RADIOPHARMACEUTICALS | EP95917659 | 1995-04-25 | EP0757694A4 | 1998-05-06 | VENKATESH MEERA; JURISSON SILVIA; SCHLEMPER ELMER; KETRING ALAN R; VOLKERT WYNN A |
| 18 | Trifunctional agents useful as irreversible inhibitors of A1-adenosine receptors | US572410 | 1990-08-24 | US5310916A | 1994-05-10 | Kenneth A. Jacobson; Gary L. Stiles; Daniel L. Boring |
| Trifunctional agents useful as inhibitors of A.sub.1 -Adenosine receptors may be formulated into pharmaceutical compositions. These agents are represented by formula (I): ##STR1## wherein X is CH or N, R is an isothiocyanate group, an amino group or --NHCO.sub.2 C(CH.sub.3).sub.3 and R.sup.1 is hydrogen, carboxyl, lower alkoxycarbonyl, aminocarbonyl, ##STR2## lower alkyl, optionally substituted with: --OH, --COOH, lower ester of COOH, carboxamide, NHCOCH.sub.3, NHCOCH.sub.2 Br, halo, dimethylamino, triethylammonium, NHCONH.sub.2, SO.sub.2 NH.sub.2, --SO.sub.3 H, or a reporter group, particularly a spectroscopic reporter group such as a fluorescent dye, photoaffinity probe, or spin label probe, coupled through an amide, sulfonamide, amine or thiourea linkage, biotinylamino- (optionally containing an .epsilon.-aminocaproyl spacer chain or similar spacer chain) or; R.sup.1 is CONH--R.sup.2 or NHCSNH--R.sup.2, wherein R.sup.2 is lower alkyl, optionally substituted with: --OH, --COOH, lower ester of COOH, carboxamide, NHCOCH.sub.3, NHCOCH.sub.2 Br, halo, dimethylamino, triethylammonium, NHCONH.sub.2, SO.sub.2 NH.sub.2, --SO.sub.3 H, or a reporter group, particularly a spectroscopic reporter group such as a fluorescent dye, photoaffinity probe, or spin label probe, coupled through an amide, sulfonamide, amine, or thiourea linkage, biotinylamino- (optionally containing an .epsilon.-aminocaproyl spacer chain or similar spacer chain). | ||||||
| 19 | Substituted thiacycloalkeno (3,2-b) pyridines and pharmaceutical compositions and method of use | US849647 | 1986-04-09 | US4705785A | 1987-11-10 | Charles F. Schwender; John H. Dodd |
| Novel substituted thiacycloalkeno [3,2-b] pyridines are described. These compounds are useful as calcium channel antagonists with cardiovascular, antiasthmatic and antibronchoconstrictor activity. | ||||||
| 20 | Sulphoxides | US804638 | 1977-06-08 | US4108866A | 1978-08-22 | Bernard Tramier; Raymond Delourme; Philippe Fresnel |
| An improved method of producing dialkyl-sulfoxides by oxidizing corresponding dialkyl-sulfides with hydrogen peroxide in aqueous acidic medium. It remedies the drawback of the similar prior art as concerns the separation of the sulfoxide formed from its reaction medium. The new method permits of easily recovering the sulfoxides in the state of good purity.The improvement consists in mixing the reaction medium with a large proportion of a solvent capable of yielding an azeotropic mixture with water. Then, after oxidization, the water is removed by distillation as azeotropic mixture. Preferably solvents are used which dissolve the dialkyl-sulfide but do not dissolve the sulfoxide formed; heptane is a particularly useful solvent. When an excess of the solvent is used, there is obtained, after distilling off the azeotropic mixture, a slurry of sulfoxide and solvent, easy to separate. | ||||||
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