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51. 发明公开

EP2349964A2 DIBENZOCYCLOHEPTANONDERIVATE UND PHARMAZEUTISCHE MITTEL, WELCHE DIESE VERBINDUNGEN ENTHALTEN 有权
标题翻译：维他命CIT，维也纳德国VERBINDUNGEN ENTHALTEN维生素DIBENZOCYCLOHEPTANONDERIVATE
公开(公告)号：EP2349964A2
公开(公告)日：2011-08-03
申请号：EP09783915.3
申请日：2009-10-09
申请人： c-a-i-r biosciences GmbH
发明人： LAUFER, Stefan , ALBRECHT, Wolfgang
IPC分类号： C07C39/42 , C07C49/747 , C07C49/755 , C07C69/16 , C07C255/22 , C07C233/33 , C07C309/65 , C07D307/12 , C07D309/12 , C07D407/10 , C07D413/12 , C07D295/088 , C07D313/12 , A61K31/35 , A61P29/00
CPC分类号： C07D295/088 , C07C49/747 , C07C49/755 , C07C205/45 , C07C205/58 , C07C205/59 , C07C225/22 , C07C229/12 , C07C229/34 , C07C271/54 , C07C309/65 , C07C2603/32 , C07D309/12 , C07D313/12 , C07D317/22 , C07D405/04
摘要： The invention relates to compounds of formula (I), in which R1, R2, R3, R4, X and Y are defined as cited in the description. The compounds have an immune-modulating action and inhibit or regulate the release of IL-1β and/or TNF-α. They can therefore be used to treat diseases that involve disorders of the immune system.
摘要翻译：二苯并环庚酮衍生物（I）及其旋光异构体，盐或溶剂化物是新的。式（I）的二苯并环庚酮衍生物及其旋光异构体，盐或溶剂化物是新的。 X，Y 1> CH 2，O，S，SO，SO 2或NR 5>; 或-X-Y 1 - ：-CH 2 -CH 2 - 或-CH = CH-; R 1>：RO，NR 6> R 7>，四唑或NR 8> CONR 13> R 14>; 任选被1,2或3个OH或1-6C-烷氧基取代的1-6C-烷基，1-6C-烷基（任选地被任选饱和的具有5或6个环原子的芳族或非芳族杂环取代并含有1个 3个杂原子，其中杂环任选被1或2个OH，1-6C-烷氧基或1-6C-烷基取代，并且可以与5或6位的苯环或任选的饱和碳环缩合具有5或6个具有1或2个O或N，1-6C-烷基，C 1-6烷基，被NR 6 R 7，CF 3 SO 2取代的C 1-6烷基的杂原子的非芳香杂环 - ，1-6C-烷基羰基氧基-1-6C-烷基或3-7C-环烷基-16C-烷基（其中环烷基残基任选地含有1或2个OH，1-6C-烷氧基或1-6C-烷基）; R 2>：H或1-6C-烷基; R 3>：式（a） - （c）的取代苯基，式（d）的取代环己烷基，NH-1-6C-亚烷基-NR 6 R 7>或四卤代; R 4>：H，卤素或1-6C-烷基; R 5> -R 7>：H或1-6C-烷基（任选被1,2或3个OH或1-6C-烷氧基取代）; R 8>：H或1-6C-烷基; R 9> -R 11>：H，NH 2，单1-6C-烷基氨基，二1-6C-烷基氨基，1-6C-烷基，1-6C-烷氧基，OH，卤素，1-6C-烷基（任选被1,2或3个卤素取代），CONR 6> R 7>或NO 2; R 12>：H或NH 2; R 13> R 14> H或C 1-6烷基; 或R 13> R 14> N：具有5或6个环原子并且具有1或2个O或N的杂原子的非芳族杂环[图像]活性：免疫调节剂; 抗炎; 平喘; 抗过敏; 抗关节炎; 抗风湿; 抗动脉硬化; 胃肠道根; 银屑病; 皮肤; 抑制细胞生长; 抗菌; 骨科; 止痛; 反病毒; Cardiant; 降血糖; Vasotropic; 内分泌根; 呼吸根; 神经保护; 同化; 精神药物; 脑保护; 嗜肝; 抗溃疡; 心血管根; CNS根; 杀病毒。作用机制：白介素-1beta抑制剂; TNF-α抑制剂。测试（I）抑制TNF-α的能力。结果表明，2-（2-氨基 - 苯基氨基）-7-（2,3-二羟基 - 丙氧基）-10,11-二氢 - 二苯并[a，d]环庚烯-5-酮显示出更大的IC 50值比5。

52. 发明公开

EP2322515A1 N-CARBOXY AMINO ACID ANHYDRIDE AND AMINO ACID CARBAMATE COMPOUND PRODUCTION METHOD 有权
标题翻译： N-羧酸氨基酸酐和氨基酸氨基甲酸酯化合物的生产方法
公开(公告)号：EP2322515A1
公开(公告)日：2011-05-18
申请号：EP09809548.2
申请日：2009-08-26
申请人： JSR Corporation
发明人： ENDO, Takeshi , KOGA, Koichi , SUDO, Atsushi
IPC分类号： C07D263/44 , C07C269/04 , C07C271/54
CPC分类号： C07D263/44 , C07C271/54 , C07C323/59
摘要： A method for production of an N-carboxy amino acid anhydride with efficiency is provided. The method for production of an N-carboxy amino acid anhydride includes a step of reaction of an amino acid organic salt compound with a carbonic acid diester.
摘要翻译：提供了一种有效生产N-羧基氨基酸酐的方法。生产N-羧基氨基酸酐的方法包括氨基酸有机盐化合物与碳酸二酯反应的步骤。

53. 发明公开

EP2322504A1 PROCESS FOR THE PREPARATION OF N-SUBSTITUTED CARBAMIC ACID ESTER AND PROCESS FOR THE PREPARATION OF ISOCYANATE USING THE N-SUBSTITUTED CARBAMIC ACID ESTER 有权转让
标题翻译：对于生产方法的N-取代氨基甲酸酯及其制造方法的异氰酸酯使用该N-取代氨基甲酸酯
公开(公告)号：EP2322504A1
公开(公告)日：2011-05-18
申请号：EP09845052.1
申请日：2009-09-29
申请人： Asahi Kasei Chemicals Corporation
发明人： MIYAKE, Nobuhisa , SHINOHATA, Masaaki , OKUBO, Atsushi
IPC分类号： C07C263/04 , C07C265/14 , C07C269/04 , C07C271/42
CPC分类号： C07C275/40 , C07C263/04 , C07C269/00 , C07C269/04 , C07C271/54 , C07C271/56 , C07C271/58 , C07C2601/14 , C07C265/14 , C07C271/52
摘要： The present invention provides a method for producing N-substituted carbamic acid-O-aryl ester derived from a compound having an ureido group, the method comprising the step of carrying out esterification or esterification and transesterification from the compound having the ureido group and a hydroxy composition containing one type or a plurality of types of hydroxy compounds.
摘要翻译：本发明提供一种生产由具有脲基的化合物衍生的N- substituiertem氨基甲酸-O-芳基酯的方法，该方法包括：从所述化合物进行酯化或酯化和酯交换具有脲基和羟基的步骤组合物含有一种类型或种类的羟基化合物的复数。

54. 发明公开

EP2322501A1 4-dedimethylamino tetracycline compounds 有权
公开(公告)号：EP2322501A1
公开(公告)日：2011-05-18
申请号：EP10183340.8
申请日：2003-01-06
申请人： Paratek Pharmaceuticals, Inc.
发明人： Nelson, Mark L. , Ohemeng, Kwasi
IPC分类号： C07C235/70 , C07C235/32 , C07D209/02 , C07D265/30 , C07D333/50 , C07D419/00 , A61K31/65 , A61P31/04
CPC分类号： A61K31/65 , C07C235/70 , C07C237/26 , C07C251/48 , C07C255/41 , C07C271/22 , C07C271/54 , C07C271/58 , C07C275/42 , C07C275/54 , C07C279/18 , C07C311/06 , C07C311/08 , C07C333/08 , C07C335/22 , C07C381/10 , C07C2601/08 , C07C2601/10 , C07C2601/16 , C07C2603/46 , C07D295/155 , C07D295/185 , C07D317/60 , C07F9/2475 , C07F9/4006
摘要： The present invention pertains, at least in part, to novel substituted 4-dedimethylamino 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.

55. 发明公开

EP2319829A1 9-substituted tetracycline compounds 审中-公开
标题翻译： 9-subsituierte四环素 - Verbindungen
公开(公告)号：EP2319829A1
公开(公告)日：2011-05-11
申请号：EP10184736.6
申请日：2004-06-25
申请人： Paratek Pharmaceuticals, Inc.
发明人： Nelson, Mark, L. , Amoo, Victor , Kim, Oak, K. , Abato, Paul , Ohemeng, Kwasi , Assefa, Haregwein , Berniac, Joel , Bhatia, Beena , Bowser, Todd , Chen, Jackson , Grier, Mark , Honeyman, Laura , Ismail, Mohamed, Y. , Mechiche, Rachid , Mathews, Jude
IPC分类号： C07C237/26 , A61K31/65
CPC分类号： C07C237/48 , A61K31/65 , C07C237/26 , C07C271/22 , C07C271/54 , C07C275/28 , C07C275/30 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2603/46
摘要： 1. A compound of formula II:

wherein:
X is CR 6' R 6 ;
R 3 is hydrogen;
R 2 , R 2' , R 5 , R 6 , R 6' , R 8 , R 10 , R 11 , and R 12 are each hydrogen;
R 4' , R 4" , R 7' and R 7" are each lower alkyl;
R 4 is NR 4 'R 4" ;
R 7 is NR 7' R 7" or hydrogen;
R 9 is -CH 2 NR 9a R 9b or linked with R 10 to form a furanyl ring;
R 9a is alkyl, alkenyl or arylalkyl; and
R 9b is hydrogen or alkyl;

or wherein R 9a and R 9b are linked to form a pyrrolidinyl, piperazinyl, piperidinyl, pyrazinyl, azapanyl, thiomorpholinyl, morpholinyl, tetrahydroquinolinyl, or decahydroquinolinyl ring;
or a pharmaceutically acceptable salt, ester or prodrug thereof.
摘要翻译： 1.式II的化合物：其中：X是CR 6'R 6; R 3是氢; R 2，R 2'，R 5，R 6，R 6'，R 8，R 10，R 11和R 12各自为氢; R 4'，R 4“，R 7'和R 7”各自为低级烷基; R 4是NR 4'R 4“; R 7是NR 7'R 7”或氢; R 9是-CH 2 NR 9a R 9b或与R 10连接以形成呋喃基环; R 9a是烷基，烯基或芳基烷基; R 9b为氢或烷基; 或其中R 9a和R 9b连接形成吡咯烷基，哌嗪基，哌啶基，吡嗪基，氮杂基，硫代吗啉基，吗啉基，四氢喹啉基或十氢喹啉基环; 或其药学上可接受的盐，酯或前药。

56. 发明公开

EP2298322A3 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：EP2298322A3
公开(公告)日：2011-05-11
申请号：EP10184642.6
申请日：2004-06-25
申请人： Paratek Pharmaceuticals, Inc.
发明人： Nelson, Mark, L. , Amoo, Victor , Kim, Oak, K. , Abato, Paul , Ohemeng, Kwasi , Assefa, Haregwein , Berniac, Joel , Bhatia, Beena , Bowser, Todd , Chen, Jackson , Grier, Mark , Honeyman, Laura , Ismail, Mohamed, Y. , Mechiche, Rachid , Mathews, Jude
IPC分类号： C07C237/26 , A61K31/65
CPC分类号： C07C237/48 , A61K31/65 , C07C237/26 , C07C271/22 , C07C271/54 , C07C275/28 , C07C275/30 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2603/46
摘要： A compound of formula III:

wherein:
X is CHC(R 13 Y'Y), CR 6' R 6 , C=CR 6' R 6 , S, NR 6 , or O;
R 2 , R 2' , R 4' , and R 4" are each independently hydrogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic, heteroaromatic or a prodrug moiety;
R 4 is NR 4' R 4" , alkyl, alkenyl, alkynyl, aryl, hydroxyl, halogen, or hydrogen;
R 2' , R 3 , R 10 , R 11 and R 12 are each hydrogen or a pro-drug moiety;
R 5 is hydroxyl, hydrogen, thiol, alkanoyl, aroyl, alkaroyl, aryl, heteroaromatic, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, alkyl carbonyloxy, or aryl carbonyloxy;
R 6 and R 6' are each independently hydrogen, methylene, absent, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
R 7 is substituted or unsubstituted pyrazolyl, furanyl, thiophenyl, thiazolyl, aminoalkyl substituted phenyl;
R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
R 9 is hydrogen;
R 13 is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl; and
Y' and Y are each independently hydrogen, halogen, hydroxyl, cyano, sulfhydryl, amino, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl, or a pharmaceutically acceptable salt thereof.
摘要翻译：式III的化合物：其中：X是CHC（R 13 Y'Y），CR 6'R 6，C = CR 6'R 6，S，NR 6或O; 烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基，芳基烷基，芳基，杂环基，杂芳基或前药部分; R4为NR4'R4“ ，烷基，烯基，炔基，芳基，羟基，卤素或氢; R2'，R3，R10，R11和R12各自为氢或前药部分; 烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基，芳基烷基，烷基羰氧基或芳基羰氧基; R 5为羟基，氢，硫醇，烷酰基，芳酰基， R6和R6'各自独立地为氢，亚甲基，不存在，羟基，卤素，硫醇，烷基，烯基，炔基，芳基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基; R7是取代或未取代的吡唑基，呋喃基，噻吩基，噻唑基，氨基烷基取代的苯基; R8为氢，羟基，卤素，硫醇，烷基，烯基，炔基，芳基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基; R9是氢; R13是氢，羟基，烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基; 和Y'和Y各自独立地为氢，卤素，羟基，氰基，巯基，氨基，烷基，链烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基，或其药学上可接受的盐。

57. 发明公开

EP2311798A1 4-dedimethylamino tetracycline compounds 审中-公开
标题翻译： 4- Dedimethylamin-Tetracyclinverbindungen
公开(公告)号：EP2311798A1
公开(公告)日：2011-04-20
申请号：EP10183323.4
申请日：2003-01-06
申请人： Paratek Pharmaceuticals, Inc.
发明人： Nelson, Mark L. , Ohemeng, Kwasi
IPC分类号： C07C235/70 , C07C235/32 , C07D209/02 , C07D265/30 , C07D333/50 , C07D419/00 , A61K31/65 , A61P31/04
CPC分类号： A61K31/65 , C07C235/70 , C07C237/26 , C07C251/48 , C07C255/41 , C07C271/22 , C07C271/54 , C07C271/58 , C07C275/42 , C07C275/54 , C07C279/18 , C07C311/06 , C07C311/08 , C07C333/08 , C07C335/22 , C07C381/10 , C07C2601/08 , C07C2601/10 , C07C2601/16 , C07C2603/46 , C07D295/155 , C07D295/185 , C07D317/60 , C07F9/2475 , C07F9/4006
摘要： The present invention pertains, at least in part, to novel substituted 4-dedimethylamino 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：本发明至少部分地涉及新的取代的4-脱二甲基氨基四环素化合物。这些四环素化合物可用于治疗多种四环素化合物反应状态，例如细菌感染和肿瘤，以及其它已知的米诺环素和四环素化合物的一般应用，例如阻断四环素外排和调节基因表达。

58. 发明公开

EP2298323A2 Substituted tetracycline compounds 审中-公开
标题翻译：取代四环素 - 维生素
公开(公告)号：EP2298323A2
公开(公告)日：2011-03-23
申请号：EP10184671.5
申请日：2004-06-25
申请人： Paratek Pharmaceuticals, Inc.
发明人： Nelson, Mark, L. , Amoo, Victor , Kim, Oak, K. , Abato, Paul , Ohemeng, Kwasi , Assefa, Haregwein , Berniac, Joel , Bhatia, Beena , Bowser, Todd , Chen, Jackson , Grier, Mark , Honeyman, Laura , Ismail, Mohamed, Y. , Mechiche, Rachid , Mathews, Jude
IPC分类号： A61K31/65 , C07C237/26 , C07D213/56 , C07D317/60 , C07D279/10 , C07D307/77 , C07D233/64 , A61P31/00 , A61P33/00
CPC分类号： C07C237/48 , A61K31/65 , C07C237/26 , C07C271/22 , C07C271/54 , C07C275/28 , C07C275/30 , C07C2601/02 , C07C2601/14 , C07C2601/16 , C07C2603/46
摘要： A compound of formula II:

wherein:
X is CHC(R 13 Y'Y), CR 6' R 6 , S, NR 6 , or O;
R 2 , R 4' , R 4" , R 7' and R 7" are each hydrogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic, heteroaromatic or a prodrug moiety;
R 4 is NR 4' R 4" , alkyl, alkenyl, alkynyl, aryl, hydroxyl, halogen, or hydrogen;
R 2' , R 3 , R 10 , R 11 and R 12 are each hydrogen or a pro-drug moiety;
R 5 is hydroxyl, hydrogen, thiol, alkanoyl, aroyl, alkaroyl, aryl, heteroaromatic, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, alkyl carbonyloxy, or aryl carbonyloxy;
R 6 and R 6' are independently hydrogen, methylene, absent, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
R 7 is NR 7' R 7" , alkyl, alkenyl, alkynyl, aryl, hydroxyl, halogen, or hydrogen;
R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
R 9 is -CH 2 NR 9a R 9b or linked with R 10 to form a furanyl ring;
R 9a is hydrogen, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, arylalkyl, aryl, heterocyclic,or heteroaromatic;
R 9b is hydrogen or alkyl;
R 8 is hydrogen, hydroxyl, halogen, thiol, alkyl, alkenyl, alkynyl, aryl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
R 13 is hydrogen, hydroxy, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl;
Y' and Y are each independently hydrogen, halogen, hydroxyl, cyano, sulfhydryl, amino, alkyl, alkenyl, alkynyl, alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkylamino, or an arylalkyl, or a pharmaceutically acceptable salt, ester or prodrug thereof.
摘要翻译：式II化合物：其中：X为CHC（R 13 Y'Y），CR 6'R 6，S，NR 6或O; R 2，R 4'，R 4“，R 7'和R 7”各自为氢，烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基，芳基烷基，芳基，杂环，杂芳族或前药部分; R 4是NR 4'R 4“，烷基，烯基，炔基，芳基，羟基，卤素或氢; R 2'，R 3，R 10，R 11和R 12各自是氢或前药部分; 烷基，链烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基，芳基烷基，烷基羰基氧基或芳基羰基氧基; R 6和R 6' 烷基，链烯基，炔基，芳基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳烷基; R 7为NR 7'R 7“，烷基，烯基，炔基，芳基，羟基，卤素或氢; R 8为氢，羟基，卤素，硫醇，烷基，烯基，炔基，芳基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基; R 9是-CH 2 NR 9a R 9b或与R 10连接以形成呋喃基环; R 9a是氢，烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基，芳烷基，芳基，杂环或杂芳族; R 9b是氢或烷基; R 8为氢，羟基，卤素，硫醇，烷基，烯基，炔基，芳基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基; R 13是氢，羟基，烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳基烷基; Y'和Y各自独立地为氢，卤素，羟基，氰基，巯基，氨基，烷基，烯基，炔基，烷氧基，烷硫基，烷基亚磺酰基，烷基磺酰基，烷基氨基或芳烷基，或其药学上可接受的盐，酯或前药。

59. 发明授权

EP1355876B1 METHODS OF CHEMICAL SYNTHESIS OF PHENOLIC NITROGEN MUSTARD PRODRUGS 有权
标题翻译：用于生产酚醛氮肥芥子气前体药物
公开(公告)号：EP1355876B1
公开(公告)日：2008-11-05
申请号：EP02715555.5
申请日：2002-01-24
申请人： The Institute of Cancer Research: Royal Cancer Hospital
发明人： SPRINGER, Caroline Joy , NICULESCU-DUVAZ, Dan
IPC分类号： C07C269/04 , C07C271/54 , C07C309/66 , C07F7/18
CPC分类号： C07F7/1852 , C07C269/04 , C07C303/28 , C07C309/66 , C07C271/54
摘要： This invention pertains to novel methods for the synthesis of certain nitrogen mustard prodrugs, such as N-{4-[N,N-bis(2-haloethylamino)-phenoxycarbonyl}-L-glutamic acid: wherein: X2 is a halo group, and is -F, -Cl, -Br, or -I; n is an integer from 0 to 4; and, each RA is an aryl substituent. The methods comprise, at least, the steps of: glutamate conjugation (GC); silyloxy deprotection (SD); and, sulfonic esterification (SU). Certain preferred methods comprise the steps of: amine substitution (AS); silyloxy protection (SP); phenolic deprotection (PD); activation (AC); glutamate conjugation (GC); silyloxy deprotection (SD); sulfonic esterification (SU); halogenation (HL); glutamate deprotection (GD); and glutamic acid protection (GP).

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