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1. 发明申请

US20160153015A1 SYNTHESIS METHOD FOR L-HETEROCYCLIC AMINO ACID AND PHARMACEUTICAL COMPOSITION HAVING THEREOF 审中-公开
标题翻译：合成氨基酸的合成方法及其具有的药物组合物
公开(公告)号：US20160153015A1
公开(公告)日：2016-06-02
申请号：US14782586
申请日：2013-06-27
申请人： ASYMCHEM LABORATORIES (TIANJIN) CO., LTD , ASYMCHEM LIFE SCIENCE (TIANJIN) CO., LTD , TIANJIN ASYMCHEM PHARMACEUTICAL CO., LTD , ASYMCHEM LABORATORIES (FUXIN) CO., LTD , JILIN ASYMCHEM LABORATORIES CO., LTD
发明人： Hao HONG , Changsheng ZHENG , Lina GUO
IPC分类号： C12P17/12 , C12P17/00 , A61K31/4409 , A61K38/44 , A61K31/4406 , A61K31/415 , A61K31/422 , C12P17/10 , A61K31/4402
CPC分类号： C12P17/12 , A61K31/415 , A61K31/422 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K38/44 , A61K48/00 , C07D213/55 , C07D231/12 , C07D333/24 , C12P13/04 , C12P13/22 , C12P17/00 , C12P17/10 , C12P41/006 , C12Y102/01002 , C12Y104/0102
摘要： A synthesis method for an L-heterocyclic amino acid and a pharmaceutical composition having the said amino acid are provided in the present disclosure. The synthesis method comprises: step A: preparing a heterocyclic keto acid, wherein the heterocycle in the heterocyclic keto acid is selected from any one of a five-membered heterocycle, a six-membered heterocycle, a seven-membered heterocycle, an alkyl-substituted five-membered heterocycle, an alkyl-substituted six-membered heterocycle, and an alkyl-substituted seven-membered heterocycle, and the keto acid group in the heterocyclic keto acid has a structural formula of and is located on any one of the carbon positions of the heterocycle, and step B: mixing the heterocyclic keto acid with ammonium formate, a phenylalanine dehydrogenase, a formate dehydrogenase and a coenzyme NAD+, and carrying out a reductive amination reaction to generate L-heterocyclic amino acid, wherein the amino acid sequence of the phenylalanine dehydrogenase is SEQ ID No. 1.
摘要翻译：在本公开内容中提供了具有所述氨基酸的L-杂环氨基酸的合成方法和药物组合物。合成方法包括：步骤A：制备杂环酮酸，其中杂环酮酸中的杂环选自五元杂环，六元杂环，七元杂环，烷基取代的五元杂环，烷基取代的六元杂环和烷基取代的七元杂环，并且杂环酮酸中的酮酸基具有结构式，位于任何一个碳位上杂环和步骤B：将杂环酮酸与甲酸铵，苯丙氨酸脱氢酶，甲酸脱氢酶和辅酶NAD +混合，并进行还原胺化反应以产生L-杂环氨基酸，其中氨基酸序列苯丙氨酸脱氢酶是SEQ ID No.1。

2. 发明申请

US20110262976A1 PRODUCTION OF R-a-LIPOIC ACID BY FERMENTATION USING GENETICALLY ENGINEERED MICROORGANISMS 审中-公开
标题翻译：通过使用遗传工程微生物发酵制备R-α-柠檬酸
公开(公告)号：US20110262976A1
公开(公告)日：2011-10-27
申请号：US12863349
申请日：2009-01-16
申请人： Mahesh Kandula , Mary E. Vaman Rao
发明人： Mahesh Kandula , Mary E. Vaman Rao
IPC分类号： C12P17/00 , C12N15/74 , C12N1/21
CPC分类号： C12P17/00 , C12N9/0008 , C12N9/1029 , C12N9/1085 , C12N9/13
摘要： This application provides systems and methods for the production of R-α-lipoic acid. Lipoic acid synthesis genes may be expressed in an acid-tolerant microorganism, such as Gluconobacter oxydans. The lipoic acid synthesis proteins may include LipA and SufE. The genetically engineered strain may be cultured under suitable culture conditions, such as in a mannitol medium with an acidic pH.
摘要翻译：该应用提供用于生产R-α-硫辛酸的系统和方法。硫辛酸合成基因可以在耐酸微生物如氧化葡糖杆菌中表达。硫辛酸合成蛋白可以包括LipA和SufE。遗传工程菌株可以在合适的培养条件下培养，例如在具有酸性pH的甘露醇培养基中。

3. 发明申请

US20100256049A1 MACROLACTONE DERIVATIVES 有权
标题翻译： MACROLACTONE衍生物
公开(公告)号：US20100256049A1
公开(公告)日：2010-10-07
申请号：US12640273
申请日：2009-12-17
申请人： Holger HOFFMANN , Christine KLEMKE-JAHN , Dietmar SCHUMMER , Herbert KOGLER
发明人： Holger HOFFMANN , Christine KLEMKE-JAHN , Dietmar SCHUMMER , Herbert KOGLER
IPC分类号： A61K38/12 , C07K5/12 , A61P31/10 , C12P21/04 , C12N1/00
CPC分类号： C07D273/00 , C07K5/0808 , C12P17/00 , C12R1/01
摘要： The disclosure relates to compounds of the formula (I): wherein R1, R2, R3, and R4 are as defined in the disclosure, or a pharmaceutically acceptable salt thereof; which is formed by the microorganism ST 201196 (DSM 18870); the use thereof for the treatment and/or prophylaxis of fungal disorders; medicaments containing a compound of formula (I); processes for production thereof; and the microorganism ST 201196 (DSM 18870).
摘要翻译：本公开涉及式（I）的化合物：其中R 1，R 2，R 3和R 4如本公开内容所定义，或其药学上可接受的盐; 其由微生物ST 201196（DSM 18870）形成; 其用于治疗和/或预防真菌病症的用途; 含有式（I）化合物的药物; 生产过程; 和微生物ST 201196（DSM 18870）。

4. 发明授权

US07785847B2 Method for producing optically active alcohols from alkanones using a dehydrogenase of azoarcus 有权
标题翻译：使用azoarcus脱氢酶从链烷醇生产光学活性醇的方法
公开(公告)号：US07785847B2
公开(公告)日：2010-08-31
申请号：US11579292
申请日：2005-05-04
申请人： Rainer Stürmer , Maria Keβeler , Bernhard Haur , Thomas Friedrich , Michael Breuer , Hartwig Schröder
发明人： Rainer Stürmer , Maria Keβeler , Bernhard Haur , Thomas Friedrich , Michael Breuer , Hartwig Schröder
IPC分类号： C12P7/22 , C12P7/04 , C12P17/00 , C12N9/04 , C12N9/14 , C12N1/20 , C07H21/04
CPC分类号： C07D333/22 , C07D333/16 , C12P17/00
摘要： The invention relates to a method for producing the optically active alkanols of formula (I), wherein n is an integer of from 0 to 5; Cyc represents an optionally substituted, mononuclear or polynuclear, saturated or unsaturated, carbocylic or heterocyclic ring, and R1 represents halogen, SH, OH, NO2, NR2R3 or NR2R3R4+X−, wherein R2, R3 and R4 independently represent H or a lower alkyl or lower alkoxy group and X− represents a counterion. According to the invention, an enzyme (E) selected from the groups of dehydrogenases, aldehyde reductases and carbonyl reductases is incubated in a medium containing the alkanone of formula (II), wherein n, Cyc and R1 are defined as above, in the presence of reduction equivalents. The compound of formula (II) is enzymatically reduced to the compound of formula (I) and the reduction equivalents consumed during reaction are regenerated by reacting a sacrificial alcohol to the corresponding sacrificial ketone using enzyme (E) and at least partially removing the sacrificial ketone from the reaction medium, and then isolating the product (I) so produced.
摘要翻译：本发明涉及一种制备式（I）的光学活性链烷醇的方法，其中n为0-5的整数; Cyc表示任选取代的单核或多核，饱和或不饱和的碳环或杂环，并且R 1表示卤素，SH，OH，NO 2，NR 2 R 3或NR 2 R 3 R 4 + X - ，其中R 2，R 3和R 4独立地表示H或低级烷基或低级烷氧基，X-表示抗衡离子。根据本发明，在含有式（II）的烷酮的培养基中温育选自脱氢酶，醛还原酶和羰基还原酶的酶的酶（E），其中n，R 1和R 1如上定义，在存在下的还原当量。将式（II）化合物酶还原成式（I）化合物，并且通过使用酶（E）使牺牲醇与相应的牺牲酮反应，并且至少部分除去牺牲酮来再生反应期间消耗的还原当量从反应介质中分离出如此制备的产物（I）。

5. 发明申请

US20100035960A1 BIOSYNTHETIC PATHWAY AND GENES REQUIRED FOR TROPODITHIETIC ACID BIOSYNTHESIS IN SILICIBACTER TM1040 有权
标题翻译：生物活性途径及其在硅胶TM1040中用于磷酸三钙生物合成的基因
公开(公告)号：US20100035960A1
公开(公告)日：2010-02-11
申请号：US12472296
申请日：2009-05-26
申请人： Robert Belas , Haifeng Geng , Ryan Powell
发明人： Robert Belas , Haifeng Geng , Ryan Powell
IPC分类号： A61K31/38 , C07H21/04 , C07K14/195 , C07D339/00 , C12P17/00 , C12N15/63
CPC分类号： C12N15/52 , A61K31/38 , C07C62/32 , C07C62/38 , C07C325/02 , C07C2601/18 , C12N15/74 , C12P17/00 , C12R1/01 , Y02A50/471
摘要： Production and use of a sulfur-containing compound, tropodithietic acid (TDA), from the roseobacter Silicibacter sp. TM1040 is described. Specifically, a biosynthetic and regulatory pathway for TDA biosynthesis in roseobacters is described. The TDA produced from roseobacters, specifically Silicibacter sp. TM1040, is shown to have antibacterial activity, in particular against Vibrio anguillarium, Vibrio cholerae, Vibrio coralliilyticus, Vibrio shiloi, Halomonas spp., Mycobacterium marinum, Mycobacterium tuberculosis, Pseudomonas elongate, Spongiobacter nikelotolerans, and Staphylococcus aureus (MRSA).
摘要翻译：生产和使用含硫化合物，二氧化二铁（TDA），来自硅酸杆菌描述TM1040。具体来说，描述了玫瑰花属中TDA生物合成的生物合成和调控途径。 TDA由玫瑰花生成，特别是Silicibacter sp。 TM1040显示具有抗菌活性，特别是针对弧菌弧菌，霍乱弧菌，弧菌弧菌，卤菌，嗜碱性分枝杆菌，结核分枝杆菌，延伸细菌，海绵状杆菌和金黄色葡萄球菌（MRSA）。

6. 发明申请

US20080319208A1 Method for Production of Optically Active (1S)-3-Chloro-1-(2-Thienyl)-Propan-1-Ol 有权
标题翻译：光活性（1S）-3-氯-1-（2-噻吩基） - 丙-1-醇的制备方法
公开(公告)号：US20080319208A1
公开(公告)日：2008-12-25
申请号：US12158526
申请日：2006-12-13
申请人： Michael Breuer
发明人： Michael Breuer
IPC分类号： C07D333/06
CPC分类号： C12P17/00 , C12P41/002
摘要： A process for preparing optically active (1S)-3-chloro-1-(2-thienyl)propan-1-ol of the formula I by, in a medium comprising 3-chloro-1-(2-thienyl)propan-1-one of the formula II reducing this compound to the compound of the formula I by means of an alcohol dehydrogenase from the Thermoanaerobacter genus, and isolating the product formed in substantially enantiomerically pure form.
摘要翻译：在包含3-氯-1-（2-噻吩基）丙-1-酮的介质中制备式I的光学活性（1S）-3-氯-1-（2-噻吩基）丙-1-醇的方法，式II的一种通过来自热厌氧杆菌属的醇脱氢酶将该化合物还原成式I的化合物，并分离基本上对映体纯的形式形成的产物。

7. 发明授权

US07052885B2 Process for preparing heterocyclic (R)- and (S)-cyanohydrins 失效
标题翻译：制备杂环（R） - 和（S） - 氰基醇的方法
公开(公告)号：US07052885B2
公开(公告)日：2006-05-30
申请号：US10325922
申请日：2002-12-23
申请人： Peter Poechlauer , Wolfgang Skranc , Herbert Mayrhofer , Irma Wirth , Rudolf Neuhofer , Herfried Griengl , Martin Fechter
发明人： Peter Poechlauer , Wolfgang Skranc , Herbert Mayrhofer , Irma Wirth , Rudolf Neuhofer , Herfried Griengl , Martin Fechter
IPC分类号： C12P17/00 , C12P17/02 , C12P17/04 , C12P17/06 , C12P17/18
CPC分类号： C12P13/004 , C12P17/00 , C12P17/04
摘要： A process for preparing enantiomer-enriched heterocyclic (R)- and (S)-cyanohydrins of the formula (I), where R1, R2, R3, R4 independently of one another are H, an unsubstituted or substituted C1–C24-alkyl, alkenyl or alkynyl radical, where one or more carbon atoms in the chain can be replaced by an oxygen atom, a nitrogen atom, a sulfur atom, an SO or an SO2 group, an unsubstituted or substituted aryl or heteroaryl radical or heterocyclic radical or halogen, hydroxyl, NR5R6, acetyl, oxo, C1–C6-carbalkoxy, C1–C6-carbalkoxyamino, COOR7, cyano, amide, benzoylamino or NO2,R5 and R6 are H, C1–C6-alkyl radical, phenyl radical, benzyl radical or COOR7, or together form a C2–C8-alkylene or heteroalkylene radical,R7 is H or C1–C6-alkyl,n is 0, 1, 2 or 3,X, Y and Z can be an unsubstituted or substituted carbon atom or a radical selected from the group consisting of N, O, S or NR5R6, where R5 and R6 are as defined above, SO or SO2, and at least one of the radicals X, Y and Z is not a carbon atom, where the compounds of the formula (I) can have one or more double bonds in the ring, with the proviso that in a 5-membered ring the double bond is not conjugated with the —C(OH)CN-group, and/or can be anellated and/or bridged,by reacting a ketone of the formula (II), where R1, R2, R3, R4, X, Y, Z and n have the meanings above, with an (R)- or (S)-hydroxynitrile lyase in an organic, aqueous or two-phase system, or in emulsion, in the presence of a cyanide group donor.
摘要翻译：制备式（I）的对映异构体富集的杂环（R） - 和（S） - 氰基醇的方法，其中R 1，R 2，R 3，R 4彼此独立地是H，未取代或取代的C 1 - 链烯基或炔基，其中链中的一个或多个碳原子可以被氧原子，氮原子，硫原子，SO或 SO 2 2基团，未取代或取代的芳基或杂芳基或杂环基或卤素，羟基，NR 5 R 6，乙酰基，氧代C 1 -C 6 - 亚烷基氧基，C 1 -C 6 - 烷氧基氨基，COOR 7，氰基，酰胺，苯甲酰氨基或NO 2，R 5和R 6是H C 1 -C 6 - 烷基，苯基，苄基或COOR 7，或一起形成C 1 -C 6 - 8亚烷基或杂亚烷基，R 7是H或C 1 -C 6 - 烷基，n是0,1,2或3，X，Y 并且Z可以是未取代或取代的碳原子或选自它的基团由N，O，S或NR5R6组成的基团，其中R 5和R 6如上定义，SO或SO 2，并且基团X，Y和Z中的至少一个不是碳原子，其中式（I）的化合物可以在环中具有一个或多个双键，条件是在5元环中双键不与-C（OH）CN-基团共轭，并且 /或可以通过使式（II）的酮（其中R 1，R 2，R 3，R 4，X，Y，Z和n具有上述含义）与（R） - 或（ S） - 羟基腈裂解酶在有机，水相或两相体系中，或在乳液中，在氰化物基团给体存在下。

8. 发明授权

US06964976B2 Amino alcohol derivatives 失效
标题翻译：氨基醇衍生物
公开(公告)号：US06964976B2
公开(公告)日：2005-11-15
申请号：US10718858
申请日：2003-11-20
申请人： Takahide Nishi , Toshiyasu Takemoto , Takaichi Shimozato , Futoshi Nara
发明人： Takahide Nishi , Toshiyasu Takemoto , Takaichi Shimozato , Futoshi Nara
IPC分类号： A61K31/381 , A61P37/06 , C07C271/16 , C07D333/20 , C07D333/22 , C07D333/32 , C07F7/18 , C12P13/00 , C12P17/00 , A61K31/42 , A61K31/135 , C07D263/04 , C07C215/00
CPC分类号： C12P13/001 , A61K31/381 , C07C271/16 , C07D333/20 , C07D333/22 , C07D333/32 , C07F7/1804 , C12P13/002 , C12P13/008 , C12P13/02 , C12P17/00 , Y02P20/55
摘要： Compounds of formula (I) which exhibit excellent immune suppression activity, pharmacologically acceptable salts thereof, esters thereof or other derivatives: wherein R1 and R2 are a hydrogen atom, an amino protecting group; R3 is a hydrogen atom, a hydroxy protecting group; R4 is a lower alkyl group; n is an integer from 1 to 6; X is an ethylene group; Y is a C1-C10 alkylene group, a C1-C10 alkylene group substituted with 1 to 3 substituents selected from substituent group a and b; R5 is an aryl group; R6 and R7 are a hydrogen atom, a group selected from substituent group a; with the proviso when R5 is a hydrogen atom, Y is not a single bond or a straight chain C1-C10 alkylene group.
摘要翻译：表现出优异的免疫抑制活性的式（I）化合物，其药理学上可接受的盐，其酯或其它衍生物：其中R 1和R 2均为氢原子，氨基保护基; R 3是氢原子，羟基保护基; R 4是低级烷基; n是1至6的整数; X是亚乙基; Y是C 1 -C 10亚烷基，C 1 -C 10亚烷基，被1个至3个选自取代基组a和b的取代基; R 5是芳基; R 6和R 7是氢原子，选自取代基a的基团; 条件是当R 5是氢原子时，Y不是单键或直链C 1 -C 10亚烷基。

9. 发明申请

US20050003496A1 Nucleic acid labeling compounds 有权
标题翻译：核酸标记化合物
公开(公告)号：US20050003496A1
公开(公告)日：2005-01-06
申请号：US10745916
申请日：2003-12-23
申请人： Glenn McGall , Anthony Barone , Handong Li
发明人： Glenn McGall , Anthony Barone , Handong Li
IPC分类号： C12P17/00 , C07
CPC分类号： C12P17/00
摘要： Nucleic acid labeling compounds containing heterocyclic derivatives are disclosed. Methods for making such heterocyclic compounds are also disclosed. The labeling compounds are suitable for enzymatic attachment to a nucleic acid, either terminally or internally, to provide a mechanism of nucleic acid detection.
摘要翻译：公开了含有杂环衍生物的核酸标记化合物。还公开了制备这种杂环化合物的方法。标记化合物适合于在末端或内部酶促附着于核酸，以提供核酸检测机制。

10. 发明申请

US20030236297A1 Amino alcohol derivatives 失效
标题翻译：氨基醇衍生物
公开(公告)号：US20030236297A1
公开(公告)日：2003-12-25
申请号：US10337702
申请日：2003-01-07
申请人： SANKYO COMPANY, LIMITED
发明人： Takahide Nishi , Toshiyasu Takemoto , Takaichi Shimozato , Futoshi Nara
IPC分类号： C07D327/10 , A61K031/381
CPC分类号： C12P13/001 , A61K31/381 , C07C271/16 , C07D333/20 , C07D333/22 , C07D333/32 , C07F7/1804 , C12P13/002 , C12P13/008 , C12P13/02 , C12P17/00 , Y02P20/55
摘要： Compounds of formula (I) which exhibit excellent immune suppression activity, pharmacologically acceptable salts thereof, esters thereof or other derivatives: 1 wherein R1 and R2 are a hydrogen atom, an amino protecting group; R3 is a hydrogen atom, a hydroxy protecting group; R4 is a lower alkyl group; n is an integer from 1 to 6; X is an ethylene group; Y is a C1-C10 alkylene group, a C1-C10 alkylene group substituted with 1 to 3 substituents selected from substituent group a and b; R5 is an aryl group; R6 and R7 are a hydrogen atom, a group selected from substituent group a; with the proviso when R5 is a hydrogen atom, Y is not a single bond or a straight chain C1-C10 alkylene group.
摘要翻译：表现出优异的免疫抑制活性的式（I）化合物，其药理学上可接受的盐，其酯或其它衍生物：其中R 1和R 2为氢原子，氨基保护基; R 3是氢原子，羟基保护基; R 4是低级烷基; n是1至6的整数; X是亚乙基; Y是C1-C10亚烷基，被1〜3个选自取代基组a和b的取代基取代的C1-C10亚烷基; R 5是芳基; R 6和R 7是氢原子，选自取代基a的基团; 条件是当R 5是氢原子时，Y不是单键或直链C1-C10亚烷基。

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