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31. 发明授权

US08933108B2 Benzothiazolone compound 有权
标题翻译：苯并噻唑酮化合物
公开(公告)号：US08933108B2
公开(公告)日：2015-01-13
申请号：US13603990
申请日：2012-09-05
申请人： Jun Cao , Bernhard Erb , Robin Alec Fairhurst , Arnaud Grandeury , Shinji Hatakeyama , Magdalena Koziczak-Holbro , Xinzhong Lai , Philipp Lustenberger , Bernd Riebesehl , Nicola Tufilli , Thomas Ullrich , Xiang Wu , Jianguang Zhou
发明人： Jun Cao , Bernhard Erb , Robin Alec Fairhurst , Arnaud Grandeury , Shinji Hatakeyama , Magdalena Koziczak-Holbro , Xinzhong Lai , Philipp Lustenberger , Bernd Riebesehl , Nicola Tufilli , Thomas Ullrich , Xiang Wu , Jianguang Zhou
IPC分类号： A01N43/78 , A61K31/425 , C07D277/62 , C07D277/68 , C07D327/04 , C07D343/00 , C07D327/10 , C07D339/02 , C07D341/00 , C07D409/00 , C07D411/00 , C07D495/00 , C07D497/00 , A61K31/428 , A61K45/06
CPC分类号： A61K31/428 , A61K31/167 , A61K45/06 , C07B2200/07 , C07C53/10 , C07D277/68 , Y02P20/55
摘要： The present invention provides a compound of formula (I) in free form or in pharmaceutically acceptable salt form a method for manufacturing the compound of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and pharmaceutical compositions.
摘要翻译：本发明提供游离形式或药学上可接受的盐形式的式（I）化合物，其制备本发明化合物的方法及其治疗用途。本发明还提供药理活性剂和药物组合物的组合。

32. 发明授权

US08691854B2 Chemical compounds and the uses thereof as a medicine 失效
标题翻译：化合物及其作为药物的用途
公开(公告)号：US08691854B2
公开(公告)日：2014-04-08
申请号：US11994354
申请日：2006-06-29
申请人： Corinne Chaimbault , Cyrille Drouot , Laure Jamot , Rebecca Pruss , Céline Simon
发明人： Corinne Chaimbault , Cyrille Drouot , Laure Jamot , Rebecca Pruss , Céline Simon
IPC分类号： A01N43/78 , A61K31/425 , C07D277/00 , C07D327/04 , C07D343/00
CPC分类号： C07D277/50
摘要： The present invention relates to the field of pharmacy, especially the treatment of neurodegenerative diseases. The invention specifically relates to a family of chemical compounds for which a neuroprotective activity has been demonstrated.Given that certain members of said family are novel compounds which have never been described, the invention relates to said novel products, the synthesis method thereof and certain novel intermediate synthesis products.The present invention further relates to compositions comprising the compounds of said family, and the use of said compounds as medicaments, especially for the preparation of a medicament for the treatment of neurodegenerative diseases.
摘要翻译：本发明涉及药学领域，特别是治疗神经变性疾病。本发明具体涉及已经证明了神经保护活性的化合物族。鉴于所述家族的某些成员是未经描述的新化合物，本发明涉及所述新产品，其合成方法和某些新型中间体合成产品。本发明还涉及包含所述家族化合物的组合物和所述化合物作为药物的用途，特别是用于制备用于治疗神经变性疾病的药物。

33. 发明授权

US08273779B2 Thiazolidin 4-one derivatives 有权
标题翻译：噻唑烷-4-酮衍生物
公开(公告)号：US08273779B2
公开(公告)日：2012-09-25
申请号：US12496945
申请日：2009-07-02
申请人： Christoph Binkert , Martin Bolli , Boris Mathys , Claus Mueller , Michael Scherz , Oliver Nayler
发明人： Christoph Binkert , Martin Bolli , Boris Mathys , Claus Mueller , Michael Scherz , Oliver Nayler
IPC分类号： A61K31/41 , A01N43/82 , C07D277/00 , C07D327/04 , C07D343/00
CPC分类号： C07D277/54 , A61K31/426 , C07D277/20 , C07D277/42 , C07D417/06
摘要： The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4-one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents.
摘要翻译：本发明涉及含有至少一种噻唑烷-4-酮衍生物以预防或治疗与活化的免疫系统相关的疾病的药物组合物。此外，本发明涉及特别用作药物活性化合物的新型噻唑烷-4-酮衍生物。所述化合物还特别用作免疫抑制剂。

34. 发明申请

US20100317725A1 Choline Esters 有权
标题翻译：胆碱酯
公开(公告)号：US20100317725A1
公开(公告)日：2010-12-16
申请号：US12815526
申请日：2010-06-15
申请人： William Garner , Margaret Garner , George Minno , Gooden David
发明人： William Garner , Margaret Garner , George Minno , Gooden David
IPC分类号： A61K31/385 , C07D339/04 , A61P27/12 , A61P27/02 , C07C53/126 , C07D343/00 , A61K31/381 , A61K31/19 , C12N5/07
CPC分类号： A61K31/385 , A61K9/0048 , A61K31/21 , C07D339/04 , C07D343/00
摘要： Compounds, formulations, and methods are provided containing the choline ester of a reducing agent, especially lipoic acid or derivatives thereof. The compounds may be administered via a topical ocular route to treat or prevent oxidative damage.
摘要翻译：提供了含有还原剂的胆碱酯，特别是硫辛酸或其衍生物的化合物，制剂和方法。化合物可以通过局部眼部途径施用以治疗或预防氧化损伤。

35. 发明申请

US20090192212A1 Dithiol Compounds, Derivatives, and Uses Therefor 有权
标题翻译：二硫醇化合物，衍生物及其用途
公开(公告)号：US20090192212A1
公开(公告)日：2009-07-30
申请号：US12390928
申请日：2009-02-23
申请人： William Garner , Margaret Garner , Ronald D. Blum
发明人： William Garner , Margaret Garner , Ronald D. Blum
IPC分类号： A61K31/095 , A61K31/382 , A61K31/385 , A61K31/381 , C07D343/00 , C07D339/08 , C07D339/06 , C07C53/00 , C07C57/13 , C07D339/04 , A61P27/02
CPC分类号： A61K31/353 , A61K31/095 , A61K31/381 , A61K31/382 , A61K31/385 , A61N5/0613 , A61N2005/067
摘要： Dithiol compounds and derivatives thereof are disclosed. The agents are useful for treating ocular disease, especially presbyopia and cataract.
摘要翻译：公开了二硫醇化合物及其衍生物。这些药剂可用于治疗眼部疾病，特别是老花眼和白内障。

36. 发明授权

US07368567B2 Arylsulfonyl benzodioxanes, benzoxazines and benzothiazines as 5-HT6 antagonists 失效
标题翻译：芳基磺酰基苯并二氧杂环己烷，苯并恶嗪和苯并噻嗪类作为5-HT6拮抗剂
公开(公告)号：US07368567B2
公开(公告)日：2008-05-06
申请号：US11121873
申请日：2005-05-04
申请人： Jacob Berger , Shu-Hai Zhao
发明人： Jacob Berger , Shu-Hai Zhao
IPC分类号： C07D265/36 , C07D498/02 , C07D321/00 , C07D323/00 , C07D327/06 , C07D327/10 , C07D339/08 , C07D341/00 , C07D343/00 , C07D409/00 , C07D411/00 , C07D495/00
CPC分类号： C07D319/20 , C07D405/06
摘要： Compounds of the formula I: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein m, n, p, Ar, X, R1, R2, R3, R4, R5 and R6 are as defined herein. Also provided are compositions comprising, methods of preparing, and methods of using the subject compounds.
摘要翻译：式I化合物或其药学上可接受的盐，溶剂合物或前药，其中m，n，p，Ar，X，R 1，R 2，R R 3，R 4，R 5和R 6如本文所定义。还提供了包含，制备方法和使用本发明化合物的方法的组合物。

37. 发明申请

US20030149093A1 (Benzodioxan, benzofuran or benzopyran) derivatives having fundic relaxation properties 有权
标题翻译：（苯并二恶烷，苯并呋喃或苯并吡喃）衍生物
公开(公告)号：US20030149093A1
公开(公告)日：2003-08-07
申请号：US10235623
申请日：2002-09-05
发明人： Piet Tom Bert Paul Wigerinck , Wim Gaston Verschueren , Marc Francis Josephine Schroven , Marcel Frans Leopold De Bruyn
IPC分类号： C07D327/06 , C07D343/00 , A61K031/38
CPC分类号： C07D405/12 , C07D405/14
摘要： The present invention of compounds of formula (I) 1 a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, wherein Alk1 is C1-6alkanediyl optionally substituted with hydroxy, C1-4alkyloxy or C1-4alkylcarbonyloxy; nullZ1nullZ2null is a bivalent radical; R1, R2 and R3 are each independently selected from hydrogen, C1-6alkyl, hydroxy, halo and the like; or when R1 and R2 are on adjacent carbon atoms, R1 and R2 taken together may form a bivalent radical; R4 is hydrogen or C1-6alkyl; A is a bivalent radical of formula nullNR6-Alk2-(b-1), or -Npiperidinyl-(CH2)m (b-2) wherein m is 0 or 1; R5 is a radical of formula 2 wherein n is 1 or 2; p1 is 0, and p2 is 1 or 2; or p1 is 1 or 2, and p2 is 0; X is oxygen, sulfur or nullNR9; Y is oxygen or sulfur; R7 is hydrogen, C1-6alkyl, C3-6cycloalkyl, phenyl or phenylmethyl; R8 is C1-6alkyl, C3-6cycloalkyl phenyl or phenylmethyl; R9 is cyano, C1-6alkyl, C3-6cyclo-alkyl, C1-6alkyloxycarbonyl or aminocarbonyl; R10 is hydrogen or C1-6alkyl; and Q is a bivalent radical. Processes for preparing said products, formulations comprising said products and their use as a medicine are disclosed, in particular for treating conditions which are related to impaired fundic relaxation.
摘要翻译：式（I）化合物的本发明是其立体化学异构形式，其N-氧化物形式或其药学上可接受的酸加成盐，其中Alk1是任选被羟基，C 1-4烷氧基或C 1-4烷基羰基氧基取代的C 1-6烷二基; -Z1-Z2-是二价基团; R 1，R 2和R 3各自独立地选自氢，C 1-6烷基，羟基，卤素等; 或当R 1和R 2在相邻碳原子上时，R 1和R 2一起可以形成二价基; R4是氢或C1-6烷基; A是式-NR6-Alk2-（b-1）或-N-哌啶基 - （CH2）m（b-2）的二价基团，其中m是0或1; R5是下式的基团，其中n为1或2; p1为0，p2为1或2; 或p1为1或2，p2为0; X为氧，硫或= NR9; Y是氧或硫; R7是氢，C1-6烷基，C3-6环烷基，苯基或苯基甲基; R8是C1-6烷基，C3-6环烷基苯基或苯基甲基; R9是氰基，C1-6烷基，C3-6环烷基，C1-6烷氧基羰基或氨基羰基; R 10是氢或C 1-6烷基; 而Q是二价基团。公开了用于制备所述产品的方法，包含所述产品的制剂及其作为药物的用途，特别是用于治疗与减退的放松有关的病症。

38. 发明授权

US5453500A Water-soluble glycosylated derivatives of 1,2-dithiin compounds 失效
标题翻译： 1,2-二硫化物化合物的水溶性糖基化衍生物
公开(公告)号：US5453500A
公开(公告)日：1995-09-26
申请号：US249492
申请日：1994-05-26
申请人： Masato Koreeda , Brian K. Shull , Wu Yang
发明人： Masato Koreeda , Brian K. Shull , Wu Yang
IPC分类号： C07H15/26 , C07D327/06 , A61K7/035 , A61K31/715 , C07D343/00
CPC分类号： C07H15/26
摘要： Novel water-soluble mono and disaccharides of 1,2-dithiins, as well as methods for their synthesis and the synthesis of 3,6-bis(hydroxymethyl)-1,2-dithiin, are provided. The water-soluble compounds have useful medicinal applications, e.g., as an antifungal agent or antibacterial agent in a pharmaceutically acceptable carrier.
摘要翻译：提供了1,2-二噻吩的新型水溶性单二糖和二糖，以及它们的合成方法和3,6-双（羟甲基）-1,2-二噻吩的合成。水溶性化合物具有有用的医学应用，例如在药学上可接受的载体中作为抗真菌剂或抗菌剂。

39. 发明授权

US5312913A Electrically conductive complex 失效
标题翻译：导电复合体
公开(公告)号：US5312913A
公开(公告)日：1994-05-17
申请号：US953746
申请日：1992-09-29
申请人： Makoto Mizutani , Kazushige Kawabata , Keiji Tanaka
发明人： Makoto Mizutani , Kazushige Kawabata , Keiji Tanaka
IPC分类号： C07D339/06 , C07D345/00 , C07D421/14 , C07D495/04 , C07D519/00 , H05K1/09 , C07D343/00 , C07D421/10
CPC分类号： C07D421/14 , C07D339/06 , C07D345/00 , C07D495/04 , H05K1/09
摘要： An electrically conductive complex obtained by reacting a thia-and/or selenafulvalenyl group-containing compound as an electron donor with an electron acceptor, and having an electron donar/electron acceptor molar ratio of 1/0.1 to 1/10, the thia-and/or selenafulvalenyl group-containing compound having the formula (I), ##STR1## wherein each of X.sub.1, X.sub.2, X.sub.3, X.sub.4, X'.sub.1, X'.sub.2, X'.sub.3 and X'.sub.4 is independently S or Se, Y is an electron donating or electron accepting group having a size which is not so large as to prevent molecular overlapping, m is an integer of 0 to 4, each of Z.sub.1, Z.sub.2, Z'.sub.1 and Z'.sub.2 is independently a hydrogen atom, C.sub.n H.sub.2n+1 in which n is an integer of 1 to 5, or alternatively, a combination of Z.sub.1 with Z.sub.2 or Z'.sub.2 and is C.sub.n H.sub.2n in which n is an integer of 1 to 5, or X(C.sub.n H.sub.2n).sub.n' X in which X is S or Se and n' is an integer of 1 to 3, and each of R.sub.1, R.sub.2, R.sub.3, R'.sub.1, R'.sub.2 and R'.sub.3 is independently a hydrogen atom or C.sub.n H.sub.2n+1 in which n is an integer of 1 to 5.
摘要翻译：一种导电络合物，其通过使具有电子给体的含硫基和/或塞来烯烯基富烯基的化合物与电子受体反应，并且具有1 / 0.1〜1/10的电子对/电子受体摩尔比，其中X 1，X 2，X 3，X 4，X'1，X'2，X'3和X'4各自为（ⅰ）独立地是S或Se，Y是具有不大于防止分子重叠的尺寸的给电子或电子接受基团，m是0至4的整数，Z1，Z2，Z'1和Z'2中的每一个独立地为氢原子，其中n为1〜5的整数的C n H 2n + 1，或者Z 1与Z 2或Z'2的组合为C n H 2n，n为1〜5的整数，X（ C n H 2n）n X，其中X为S或Se，n'为1〜3的整数，R1，R2，R3，R'1，R'2和R'3各自独立地为氢原子或Cn H2n + 1，其中n为1〜5的整数。

40. 发明授权

US4312992A Substituted heterofulvalenes 失效
标题翻译：取代的杂多异戊烯
公开(公告)号：US4312992A
公开(公告)日：1982-01-26
申请号：US74927
申请日：1979-09-13
申请人： Dennis C. Green
发明人： Dennis C. Green
IPC分类号： C07D339/04 , C07D345/00 , H01G9/02 , H01G9/028 , H01M6/18 , C07D339/06 , C07D343/00
CPC分类号： H01G9/028 , C07D339/04 , C07D345/00 , H01M6/18
摘要： Substituted derivatives of tetrathiafulvalene, tetraselenafulvalene and dithiadiselenafulvalene having the general formulae ##STR1## where Z is S and Y is S; Z is S and Y is Se; and Z is Se and Y is Se, and R can be CO.sub.2 H, R'R"COH, R'CHOH, COR', SCH.sub.3, SO.sub.2.sup.- Li.sup.+, SnR.sub.3 ', SiR.sub.3, --CH.sub.2 OH --CO.sub.2 R', R'CHOH, CHO, CR.sub.2 ' CR.sub.2 'OH, TTF, TSeF and DTDSeF, R' and R" can be the same or different and is selected from the group consisting of alkyls, aryls, alkaryls, ether substituted alkyls, halogen substituted alkyls and halogens, are prepared. A novel method for their preparation is also described.
摘要翻译：具有通式的四硫富瓦烯，四硫代富瓦烯和二硫杂十一烯的富瓦烯的取代衍生物，其中Z是S，Y是S; Z为S，Y为Se; Z为Se且Y为Se，R为CO 2 H，R'R''COH，R'CHOH，COR'，SCH3，SO2-Li +，SnR3'，SiR3，-CH2OH-CO2R'，R'CHOH， CHO，CR2'CR2'OH，TTF，TSeF和DTDSeF，R'和R“可以相同或不同，并且选自烷基，芳基，烷芳基，醚取代的烷基，卤素取代的烷基和卤素，准备好了还描述了一种其制备方法。

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