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1. 发明公开

EP2481723A2 Substituted tetracycline compounds 审中-公开
标题翻译：被取代的四环素化合物
公开(公告)号：EP2481723A2
公开(公告)日：2012-08-01
申请号：EP12158471.8
申请日：2003-03-18
申请人： Paratek Pharmaceuticals, Inc.
发明人： The designation of the inventor has not yet been filed
IPC分类号： C07C237/26 , A61K31/65 , A61P31/00
CPC分类号： C07D307/52 , C07C237/26 , C07C239/18 , C07C251/08 , C07C251/48 , C07C255/25 , C07C255/43 , C07C255/58 , C07C255/59 , C07C271/28 , C07C271/44 , C07C275/34 , C07C279/18 , C07C281/14 , C07C309/61 , C07C311/19 , C07C311/21 , C07C317/48 , C07C323/32 , C07C323/60 , C07C2603/46 , C07D207/16 , C07D211/58 , C07D213/30 , C07D213/61 , C07D213/65 , C07D213/75 , C07D239/26 , C07D239/30 , C07D239/42 , C07D261/10 , C07D261/18 , C07D295/108 , C07D295/155 , C07D295/215 , C07D307/28 , C07D307/68 , C07D317/54 , C07D401/04
摘要： The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.
摘要翻译：本发明至少部分涉及新的取代的四环素化合物。这些四环素化合物可用于治疗许多四环素化合物反应性状态，例如细菌感染和肿瘤，以及其他一般的米诺环素和四环素化合物的应用，例如阻断四环素外排和基因表达的调节。

2. 发明公开

EP0832875A1 HIGHLY WATER-SOLUBLE METALLOPROTEINASE INHIBITOR 失效
标题翻译：在WASSERHOCHLÖSLICHERMETALLOPROTEINASE-INHIBITOR
公开(公告)号：EP0832875A1
公开(公告)日：1998-04-01
申请号：EP96912242.3
申请日：1996-04-25
申请人： FUJI YAKUHIN KOGYO KABUSHIKI KAISHA
发明人： FUJISAWA, Tetsunori-Fuji Yakuhin Kogyo Kabushiki , ODAKE, Shinjiro-Fuji Yakuhin Kogyo Kabushiki , MORITA, Yasuo-Fuji Yakuhin Kogyo Kabushiki , HONGO, Tomoko-Fuji Yakuhin Kogyo Kabushiki , ITO, Hajime-Fuji Yakuhin Kogyo Kabushiki Kaisha , YASUDA, Junko-Fuji Yakuhin Kogyo Kabushiki Kaisha , SUDA, Eiko-Fuji Yakuhin Kogyo Kabushiki Kaishanai , IGETA, Katsuhiro-Fuji Yakuhin Kogyo Kabushiki K. , MORIKAWA, Tadanori-Fuji Yakuhin Kogyo Kabushiki
IPC分类号： C07C237/20 , C07C237/22 , C07C259/06 , C07C309/61 , C07D521/00 , C07F7/18 , C07F9/09 , A61K31/165 , A61K31/33 , A61K31/66 , C12N9/99
CPC分类号： C07C323/60 , A61K31/165 , C07C239/06 , C07C259/06 , C07C279/14 , C07C279/16 , C07C305/24 , C07C309/61 , C07F9/12
摘要： New compounds of the general formula (I)
(wherein R 1 is a hydrogen atom, or a hydroxyl, aryl(C 1 -C 6 )alkylene or -A-SO -B group (A is a (C 1 -C 6 ) alkylene group; B is a (C 1 -C 6 ) alkyl, (C 1 -C 6 ) acyl, aryl or heterocyclyl group; n is 0, 1 or 2), R 2 is a hydrogen atom, or a (C 1 -C 6 ) alkyl, (C 1 -C 6 ) alkyloxy or (C 1 -C 6 ) alkylthio group, R 3 and R 4 are identical or different, representing a hydrogen atom, or a (C 1 -C 6 ) alkyl, aryl or aryl(C 1 -C 6 )alkylene group, R 5 is a -Y-C or C group (Y is a (C 1 -C 6 ) alkylene group, an oxygen atom, an imino group or a (C 1 -C 6 ) alkyleneimino group, C is a sulfonic acid, phosphonic acid, amidino, (C 1 -C 6 ) acyl, acylimidoyl, diphosphonomethine or dicarboxymethine group), and R 6 is a hydrogen atom, or a nonsubstituted or substituted benzyl, trialkylsilyl, tert-butyldiphenylsilyl, tetrahydropyranyl or tert-butyl group) or stereoisomers thereof, and pharmaceutically acceptable salts thereof and solvates thereof, and the process for the preparation thereof, and metalloproteinase inhibitors which comprise one or more compounds selected from those compounds as effective ingredients and inhibit matrix metalloproteinases (MMPs) and/or TNF-α converting enzyme. Furthermore, the preparation intermediates to obtain the compounds of the formula (I) and the process for the preparation.
摘要翻译：通式（I）的新化合物（其中R 1为氢原子，或羟基，芳基（C 1 -C 6）亚烷基或-A-SO b -B基（A为（C1- C6）亚烷基; B是（C1-C6）烷基，（C1-C6）酰基，芳基或杂环基; n是0,1或2），R 2是氢原子或（C1- C 1 -C 6）烷基，（C 1 -C 6）烷氧基或（C 1 -C 6）烷硫基，R 3和R 4相同或不同，表示氢原子或（C 1 -C 6）烷基，芳基或芳基（C 1 -C 6）亚烷基，R 5为-YC或C基（Y为（C1-C6）亚烷基，氧原子，亚氨基或（C1-C6）亚烷基亚氨基），C为磺酸，膦酸，脒基，（C 1 -C 6）酰基，酰亚氨基，二膦酰甲基或二羧基甲基），R 6是氢原子，或非取代或取代的苄基，三烷基甲硅烷基，叔丁基二苯基甲硅烷基，四氢吡喃基或叔 - 丁基）或其立体异构体及其药学上可接受的盐及其溶剂化物，及其制备方法和金属蛋白酶抑制剂，其包含一种或多种选自那些化合物的化合物作为有效成分并抑制基质金属蛋白酶（MMPs）和/或TNF-α转化酶。此外，制备中间体以获得式（I）化合物及其制备方法。

3. 发明授权

EP0799195B1 PROCESS FOR THE PREPARATION OF AROMATIC O-SULFOCARBOXYLIC ACIDS AND SULFONYLUREAS 失效
标题翻译： PROCESS FOR磺酰脲类药物生产芳香O型磺酸羧酸
公开(公告)号：EP0799195B1
公开(公告)日：1999-04-14
申请号：EP95941086.1
申请日：1995-12-11
申请人： Novartis AG
发明人： SIEGRIST, Urs , MÜLLER, Manfred , BRÜNISHOLZ, Jean
IPC分类号： C07C303/22 , C07D521/00
CPC分类号： C07D405/12 , C07C303/22 , C07C309/60 , C07C309/61
摘要： The invention relates to a process for the preparation of ortho-sulfocarboxylic acids of formula (I), which comprises: a) in a first reaction step, diazotising an aromatic ortho-aminosulfonic acid in the presence of an acid and nitrite in water, in an organic solvent or in a mixture thereof, to an ortho-diazonium sulfonate, and, b) in a second reaction step, reacting the ortho-diazonium sulfonate in the presence of a palladium catalyst in water, in an organic solvent or in a mixture thereof, with carbon monoxide, under overpressure, to an aromatic ortho-sulfocarboxylic acid. The invention also relates to a process for the preparation of sulfonylureas of formula (II) using ortho-sulfocarboxylic acids as intermediates.

4. 发明公开

EP0733036A1 ALPHA-QUATERNARY-ALPHA-AMINO ACIDS FOR USE AS CNS AGENTS 失效
标题翻译： ALPHA-季α-氨基酸FOR USE AS ACTIVE对中枢神经系统
公开(公告)号：EP0733036A1
公开(公告)日：1996-09-25
申请号：EP95903410.0
申请日：1994-12-09
申请人： UNIVERSITY OF BRISTOL , Tocris Cookson Limited
发明人： WATKINS, Jeffrey, Clifton 8 Lower Court Road , JANE, David, Edward
IPC分类号： C07C229 , C07C309 , C07F9
CPC分类号： C07F9/301 , C07C229/24 , C07C229/46 , C07C309/61 , C07C2601/02 , C07F9/091 , C07F9/3808
摘要： Compounds of formula (I) are disclosed wherein: Y is selected from carboxy, phosphono, -PO2H(OR13), phosphinico, -PO¿2H(R?13), -OPO¿3?H2, -OPO2H(OR?13¿), arsono, -AsO¿2H(OR?13), arsinico, -AsO¿2H(R?13), sulpho, sulphino, sulpheno, OSO¿3?H, tetrazolyl, 3-hydroxyisoxazole, 1,2,4-oxadiazolidin-3,5-dione and hydantoin where R?13 is C¿1 to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkylene or optionally substituted aryl or aralkyl; B is selected from C1 to C8 alkylene, C3 to C8 cycloalkylene, C2 to C8 alkenylene and C2 to C8 alkynylene optionally chain substituted and optionally substituted on the chain; Q is selected from carboxy, C1 to C6 alkoxycarbonyl and hydroxamic acid; R10 is selected from C¿1? to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C3 to C8 cycloalkylene, haloalkyl and optionally substituted aryl, aralkyl or biaryl; and R?11 and R12¿ are the same or different and are selected from hydrogen, C¿1? to C6 alkyl, C2 to C6 alkenyl, C2 to C6 alkynyl, C1 to C6 acyl and optionally substituted benzoyl, two of Y, Q, R?10, R11, R12¿ and the substituents on B being optionally condensed with each other to form a carbocyclic or heterocyclic ring system, and pharmaceutically acceptable salts thereof. The compounds may be used as agents to influence the central nervous system.
摘要翻译：式（I）化合物是游离缺失盘worin：Y选自羧基，膦酰基，-PO 2 H所选（或<13>），磷酸亚基，-PO 2 H（R <13>），-OPO 3 H 2，-OPO2H（OR <13>） arsono，-AsO2H（OR <13>），arsinico，-AsO2H（R <13>），磺基，sulphino，sulpheno，OSO 3 H，四唑基，3-羟基异，1,2,4-恶二唑烷-3,5-二酮和乙内酰脲，其中R <13>是C1-C6烷基，C2至C6烯基，C2至C6炔基，C3-C8的亚环烷基或任选取代的芳基或芳烷基; 乙选自C1至C8亚烷基，C3至C8亚环烷基，C2至C8链烯基和C2至C8亚炔基链任选substituiertem并且在链任选substituiertem; Q选自羧基选择，C1至C6烷氧基羰基和异羟肟酸; [R <10>选自C1至C6烷基，C2至C6烯基，C2至C6炔基，C3-C8的亚环烷基，卤代烷基和任选地substituiertem芳基，芳烷基或二芳基; 且R <11>和R <12>是相同的或不同的，选自氢，C1-C6烷基，C2至C6烯基，C2到C6炔基，C1至C6酰基和任选substituiertem苯甲酰基，两个Y，Q的，R <10>，R <11>，R <12>和B上的取代基任选被海誓山盟冷凝以形成碳环或杂环体系，和其可药用盐。这些化合物可以用作药物来影响中枢神经系统。

5. 发明公开

EP1660011A2 ARYL, HETEROAROMATIC AND BICYCLIC ARYL NITRONE COMPOUNDS, PRODRUGS AND PHARMACEUTICAL COMPOSITIONS OF THE SAME TO TREAT HUMAN DISORDERS 审中-公开
标题翻译：芳基，杂芳族和双环芳基硝酮化合物，前体药物及其药物组合物用于治疗人的疾病
公开(公告)号：EP1660011A2
公开(公告)日：2006-05-31
申请号：EP04780091.7
申请日：2004-08-04
申请人： Renovis, Inc.
发明人： KELLY, Michael, G. , JANAGANI, Satyanarayana , UPASANI, Ravindra, B.
IPC分类号： A61K6/00
CPC分类号： C07C291/02 , C07C309/46 , C07C309/61 , C07C309/76 , C07C311/16 , C07C323/47 , C07C2601/02 , C07C2601/08 , C07C2601/14 , C07D209/42 , C07D213/65 , C07D213/70 , C07D213/74 , C07D213/75 , C07D215/36 , C07D231/12 , C07D233/06 , C07D295/135 , C07D333/38 , C07F9/3856 , C07F9/4021
摘要： Disclosed are aryl, heteroaromatic and bicyclic aryl nitrone compounds and pharmaceutical compositions containing such derivatives. The disclosed compositions are useful for preventing and/or treating pain, neurodegenerative, autoimmune and inflammatory diseases or conditions in mammals.
摘要翻译：公开的是芳基，杂芳族和双环芳基硝酮化合物和含有寻求衍生物的药物组合物。盘游离缺失的组合物是用于预防和/或治疗疼痛，神经变性，自身免疫和炎性疾病或病症在哺乳动物中是有用的。

6. 发明公开

EP1503981A2 SUBSTITUTED TETRACYCLINE COMPOUNDS 审中-公开
标题翻译：取代的四环素
公开(公告)号：EP1503981A2
公开(公告)日：2005-02-09
申请号：EP03714236.1
申请日：2003-03-18
申请人： Paratek Pharmaceuticals, Inc.
发明人： NELSON, Mark, L. , OHEMENG, Kwasi , FRECHETTE, Roger , ABATO, Paul , ASSEFA, Haregewein , BANDARAGE, Upul , BERNIAC, Joel , BHATIA, Beena , CHEN, Jackson , ISMAIL, Mohamed, Y. , KIM, Oak, A. , MATHEWS, Jude , HONEYMAN, Laura , NIHLAWI, Mohammed , PEARSON, Andre , REDDY, Laxma , SHEAHAN, Paul , SIZENSKY, Emmanuelle , TOURIGNY, Justin , VISKI, Peter , WARCHOL, Tadeusz , AMOO, Victor , MECHICHE, Rachid , VERMA, Atul K.
IPC分类号： C07C237/26 , C07C43/00 , C07C49/00
CPC分类号： C07D307/52 , C07C237/26 , C07C239/18 , C07C251/08 , C07C251/48 , C07C255/25 , C07C255/43 , C07C255/58 , C07C255/59 , C07C271/28 , C07C271/44 , C07C275/34 , C07C279/18 , C07C281/14 , C07C309/61 , C07C311/19 , C07C311/21 , C07C317/48 , C07C323/32 , C07C323/60 , C07C2603/46 , C07D207/16 , C07D211/58 , C07D213/30 , C07D213/61 , C07D213/65 , C07D213/75 , C07D239/26 , C07D239/30 , C07D239/42 , C07D261/10 , C07D261/18 , C07D295/108 , C07D295/155 , C07D295/215 , C07D307/28 , C07D307/68 , C07D317/54 , C07D401/04
摘要： The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.

7. 发明公开

EP3143022A1 CARBOPYRONONE COMPOUNDS USEFUL AS DIAGNOSTIC ADJUVANTS 审中-公开
标题翻译：用作诊断佐剂的羰基硼氢化合物化合物
公开(公告)号：EP3143022A1
公开(公告)日：2017-03-22
申请号：EP15725202.4
申请日：2015-05-15
申请人： Life Technologies Corporation
发明人： GEE, Kyle , KANG, Hee Chol , ZHOU, Wenjun , DUBBELS, Bradley , OLSZOWY, Michael , O'GRADY, Michael
IPC分类号： C07D471/04 , C07C251/24
CPC分类号： G01N33/5005 , C07C309/61 , C07C2603/24 , C07D471/04 , C07K16/2812 , C09B11/28 , G01N33/5014 , G01N33/5044
摘要： Described herein are fluorescent compounds and methods and comprising these compounds. The compounds disclosed herein are carbopyronine reagents that fluoresce in the red portion of the UV/VIS spectrum and provide bright fluorescence intensity, uniform cell staining, and good retention within live cells as well as low toxicity toward cells.
摘要翻译：本文描述了荧光化合物和方法并且包含这些化合物。本文公开的化合物是卡比洛啉试剂，其在UV / VIS光谱的红色部分发荧光并且提供明亮的荧光强度，均匀的细胞染色，以及在活细胞内的良好保留以及对细胞的低毒性。

8. 发明授权

EP0832875B1 HIGHLY WATER-SOLUBLE METALLOPROTEINASE INHIBITOR 失效
标题翻译：高度溶于水金属蛋白酶抑制剂
公开(公告)号：EP0832875B1
公开(公告)日：2004-06-30
申请号：EP96912242.3
申请日：1996-04-25
申请人： Daiichi Fine Chemical Co., Ltd.
发明人： FUJISAWA, Tetsunori Daiichi Fine Chemical Co.,Ltd. , ODAKE, Shinjiro Daiichi Fine Chemical Co.,Ltd. , MORITA, Yasuo Daiichi Fine Chemical Co.,Ltd. , HONGO, Tomoko Daiichi Fine Chemical Co.,Ltd , ITO, Hajime Daiichi Fine Chemical Co.,Ltd. , YASUDA, Junko Daiichi Fine Chemical Co.,Ltd. , SUDA, Eiko Daiichi Fine Chemical Co.,Ltd. , IGETA, Katsuhiro Daiichi Fine Chemical Co.,Ltd. , MORIKAWA, Tadanori Daiichi Fine Chemical Co.,Ltd.
IPC分类号： C07C237/20 , C07C237/22 , C07C259/06 , C07C309/61 , C07D521/00 , C07F7/18 , C07F9/09 , A61K31/165 , A61K31/33 , A61K31/66 , C07C239/06 , C07C279/16 , C07F9/12 , C07C323/60 , C07C279/14 , C07C305/24
CPC分类号： C07C323/60 , A61K31/165 , C07C239/06 , C07C259/06 , C07C279/14 , C07C279/16 , C07C305/24 , C07C309/61 , C07F9/12
摘要： Novel compounds represented by general formula (I), stereoisomers thereof, pharmaceutically acceptable salts, and solvates thereof, processes for the preparation thereof, a matrix metalloproteinase inhibitor comprising as the active ingredient at least one member selected among the above compounds, intermediates for preparing the compounds represented by general formula (I), and a process for preparing the same.

9. 发明公开

EP1289936A1 SUBSTITUTED STILBENES AS GLUCOSE UPTAKE ENHANCERS 有权
标题翻译：取代芪葡萄糖录音抑制剂
公开(公告)号：EP1289936A1
公开(公告)日：2003-03-12
申请号：EP01941753.4
申请日：2001-06-01
申请人： TELIK, INC.
发明人： PATTERSON, John , PARK, Jeong, Weong , LUM, Robert, T. , SPEVAK, Wayne, R.
IPC分类号： C07C237/42 , C07C237/40 , C07C233/81 , C07C235/56 , C07C309/61 , A61K31/196 , A61K31/24 , C07C231/02
CPC分类号： C07C233/81 , C07C233/88 , C07C235/56 , C07C235/64 , C07C235/84 , C07C237/40 , C07C237/42 , C07C309/51 , C07C309/61 , C07D317/60
摘要： The present invention relates to chemical compounds, pharmaceutical compositions comprising said compounds, methods of treatment administering these compounds to mammalian hosts, and processes for their preparation. Specifically, the invention relates to a means to enhance insulin-dependent glucose uptake. More specifically, the invention concerns compounds and pharmaceutical compositions that activate the insulin receptor kinase, which leads to increased sensitivity to insulin and an increase in glucose uptake, as well as processes for the preparation of the compounds. The invention also specifically concerns methods for treating humans with hyperglycemia, especially for the treatment of Type II diabetes.

10. 发明公开

EP0502893A1 AZOVERBINDUNGEN UND IHRE VERWENDUNG ALS FARBSTOFFE, 1-SULFO-6-CARBOXY-2-AMINO-NAPHTHALIN, DESSEN VERWENDUNG ALS DIAZOKOMPONENT UND VERFAHREN ZUR HERSTELLUNG DIESER VERBINDUNGEN 失效
标题翻译：偶氮化合物及其作为活性染料使用，1-磺化-6-羧基-2-氨基萘，其作为DIAZOKOMPONENT AND METHOD FOR PRODUCING这些化合物。
公开(公告)号：EP0502893A1
公开(公告)日：1992-09-16
申请号：EP90917303.0
申请日：1990-11-26
申请人： HOECHST AKTIENGESELLSCHAFT
发明人： SPRINGER, Hartmut , HUSSONG, Kurt
IPC分类号： C07D231 , C07C309 , C09B29 , C09B62 , D06P1
CPC分类号： C07C309/61 , C09B29/0014 , C09B62/507
摘要： L'invention décrit des composés azoïques qui correspondent à la formule générale (1) mentionnée ci-après, possèdent des qualités fibroréactives et représentent des colorants appréciables. Ils colorent une matière synthétique et naturelle contenant des groupes hydroxy- et/ou carbonamide, particulièrement des matières fibreuses comme la laine et particulièrement des matières de fibres cellulosiques, en des tons intenses. La formule (1) où: M est hydrogène ou un métal salifiant tel qu'un métal alcalin; K° est un résidu de formules générales (2A) ou (2B) dans lesquelles E est le résidu d'un agent usuel dans les colorants disazoïques pouvant servir aussi bien de composant de copulation que de composant diazoïque, comme par exemple le résidu d'un composé 1-(aminophényle -ou- aminonaphtyle) -pyrazolone-, aminonaphtol-, aniline- ou 1-aminonaphtaline, v est zéro ou 1, K est le résidu d'un composant de copulation soluble à l'eau, de préférence à partir de la série naphtol-, aminonaphtol, aniline-, pyrazolone, hydroxypyridone- et acétoacétyl- arylide, ce composant de copulation contenant 1 ou 2 groupes fibroréactifs de la série sulfone de vinyle, D est un résidu de benzol ou naphtaline, ses substituants R1 et R2 étant des substituants usuels dans les colorants azoïques comme, par exemple (outre l'hydrogène) alkyle inférieur, alcoxy inférieur, halogène, sulfo et carboxy, le groupe -SO2-Y est un groupe fibroréactif de la série sulfone de vinyle, a est zéro, 1 ou 2 et k est 1 ou 2. On décrit de plus le composé 2-amino-naphthaline-1-acide sulfonique-6-acide carbonique, qui peut servir de pré-produit pour la fabrication de colorants, comme, à titre d'exemple, constituant diazoïque pour la synthèse des colorants de la formule générale (1).

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