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1. 发明授权

US07582668B2 Imidazoyl-benzamide anti-cancer agents 有权
标题翻译：咪唑酰苯甲酰胺抗癌剂
公开(公告)号：US07582668B2
公开(公告)日：2009-09-01
申请号：US11598250
申请日：2006-11-08
申请人： Xiangping Qian , Luke W. Ashcraft , Jianchao Wang , Bing Yao , Hong Jiang , Gustave Bergnes , Bradley P. Morgan , David J. Morgans, Jr. , Dashyant Dhanak , Steven D. Knight , Nicholas D. Adams , Cynthia A. Parrish , Kevin J. Duffy , Duke Fitch , Rosanna Tedesco
发明人： Xiangping Qian , Luke W. Ashcraft , Jianchao Wang , Bing Yao , Hong Jiang , Gustave Bergnes , Bradley P. Morgan , David J. Morgans, Jr. , Dashyant Dhanak , Steven D. Knight , Nicholas D. Adams , Cynthia A. Parrish , Kevin J. Duffy , Duke Fitch , Rosanna Tedesco
IPC分类号： A61K31/4178 , C07D403/10
CPC分类号： C07D233/64 , C07C235/48 , C07C235/50 , C07C235/52 , C07C237/22 , C07C255/57 , C07C255/59 , C07C255/60 , C07C257/08 , C07C257/18 , C07C259/18 , C07C271/20 , C07C271/24 , C07C271/28 , C07C275/26 , C07C275/40 , C07C275/42 , C07C281/06 , C07C307/10 , C07C311/37 , C07C311/46 , C07C2601/02 , C07C2601/14 , C07D207/273 , C07D211/34 , C07D211/76 , C07D213/30 , C07D231/12 , C07D231/14 , C07D233/61 , C07D233/70 , C07D235/06 , C07D235/16 , C07D235/18 , C07D235/26 , C07D239/36 , C07D249/08 , C07D257/04 , C07D261/08 , C07D263/10 , C07D263/12 , C07D263/32 , C07D271/06 , C07D271/07 , C07D271/10 , C07D271/113 , C07D277/30 , C07D277/42 , C07D277/56 , C07D285/02 , C07D285/125 , C07D295/145 , C07D295/155 , C07D333/38 , C07D403/10 , C07D403/12 , C07D413/06 , C07D471/04 , C07D498/04 , C07F9/6506 , C07F9/6561
摘要： Provided are compounds of Formula I and pharmaceutically acceptable salts thereof which may be useful for the treatment of cancer or other proliferative disorders.
摘要翻译：提供了可用于治疗癌症或其它增殖性疾病的式I化合物及其药学上可接受的盐。

2. 发明申请

US20080255182A1 Certain chemical entities, compositions, and methods 审中-公开
标题翻译：某些化学实体，组合物和方法
公开(公告)号：US20080255182A1
公开(公告)日：2008-10-16
申请号：US12007143
申请日：2008-01-07
申请人： Xiangping Qian , Andrew I. McDonald , Han-Jie Zhou , Luke W. Ashcraft , Bing Yao , Hong Jiang , Jennifer Kuo Chen Huang , Jianchao Wang , David J. Morgans , Bradley P. Morgan , Gustave Bergnes , Dashyant Dhanak , Steven D. Knight , Nicholas D. Adams , Cynthia A. Parrish , Kevin Duffy , Duke Fitch , Rosanna Tedesco
发明人： Xiangping Qian , Andrew I. McDonald , Han-Jie Zhou , Luke W. Ashcraft , Bing Yao , Hong Jiang , Jennifer Kuo Chen Huang , Jianchao Wang , David J. Morgans , Bradley P. Morgan , Gustave Bergnes , Dashyant Dhanak , Steven D. Knight , Nicholas D. Adams , Cynthia A. Parrish , Kevin Duffy , Duke Fitch , Rosanna Tedesco
IPC分类号： A61K31/437 , A61P35/00
CPC分类号： C07D233/64 , C07C235/48 , C07C235/50 , C07C235/52 , C07C237/22 , C07C255/57 , C07C255/59 , C07C255/60 , C07C257/08 , C07C257/18 , C07C259/18 , C07C271/20 , C07C271/24 , C07C271/28 , C07C275/26 , C07C275/40 , C07C275/42 , C07C281/06 , C07C307/10 , C07C311/37 , C07C311/46 , C07C2601/02 , C07C2601/14 , C07D207/273 , C07D211/34 , C07D211/76 , C07D213/30 , C07D231/12 , C07D231/14 , C07D233/61 , C07D233/70 , C07D235/06 , C07D235/16 , C07D235/18 , C07D235/26 , C07D239/36 , C07D249/08 , C07D257/04 , C07D261/08 , C07D263/10 , C07D263/12 , C07D263/32 , C07D271/06 , C07D271/07 , C07D271/10 , C07D271/113 , C07D277/30 , C07D277/42 , C07D277/56 , C07D285/02 , C07D285/125 , C07D295/145 , C07D295/155 , C07D333/38 , C07D403/10 , C07D403/12 , C07D413/06 , C07D471/04 , C07D498/04 , C07F9/6506 , C07F9/6561
摘要： Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of one or more mitotic kinesins are disclosed.
摘要翻译：公开了通过调节一种或多种有丝分裂驱动蛋白的活性来治疗细胞增殖性疾病和病症的化合物。

4. 发明授权

US07115769B2 Synthesis of 2-alkylcysteine via phase transfer catalysis 有权
公开(公告)号：US07115769B2
公开(公告)日：2006-10-03
申请号：US10438757
申请日：2003-05-15
申请人： Rayomand H. Gimi , Mukund S. Chorghade
发明人： Rayomand H. Gimi , Mukund S. Chorghade
IPC分类号： C07C323/52
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. In one embodiment, the present invention provides methods of preparing 2-alkylcysteine derivatives. In another embodiment, the method comprises forming a 2-alkylcysteine derivative from a cysteine derivative in the presence of a phase transfer catalyst. In particular, the present invention provides methods for preparing 2-methylcysteine derivatives.The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In one aspect, an aryl nitrile or imidate is condensed with cysteine or a 2-alkyl cysteine. The present invention also relates to the preparation of 4,5-dihydro-2-(2,4-dihydroxyphenyl)-4-alkyl-thiazole-4-carboxylic acids, such as 4,5-dihydro-2-(2,4-dihydroxyphenyl)-4-methyl-thiazole-4-carboxylic acid.

5. 发明授权

US07002036B2 Synthesis of 2-alkyl amino acids 失效
公开(公告)号：US07002036B2
公开(公告)日：2006-02-21
申请号：US10438770
申请日：2003-05-15
申请人： Mukund S. Chorghade , Mukund K. Gurjar , Debendra K. Mohapatra
发明人： Mukund S. Chorghade , Mukund K. Gurjar , Debendra K. Mohapatra
IPC分类号： C07C34/00
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.

6. 发明授权

US06903220B2 Synthesis of chiral 2-alkyl amino acids 有权
标题翻译：手性2-烷基氨基酸的合成
公开(公告)号：US06903220B2
公开(公告)日：2005-06-07
申请号：US10439313
申请日：2003-05-15
申请人： Mukund S. Chorghade , Mukund K. Gurjar , Bhanu M. Chanda
发明人： Mukund S. Chorghade , Mukund K. Gurjar , Bhanu M. Chanda
IPC分类号： C07D233/64 , A61K31/426 , A61P7/02 , A61P11/06 , A61P29/00 , A61P31/12 , C07B53/00 , C07B55/00 , C07B61/00 , C07C217/46 , C07C227/18 , C07C229/06 , C07C229/42 , C07C249/02 , C07C253/00 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07C323/00 , C07C323/25 , C07C323/35 , C07C323/52 , C07C323/56 , C07C323/58 , C07D213/55 , C07D233/16 , C07D237/02 , C07D277/04 , C07D277/08 , C07D277/12 , C07D277/14 , C07D277/18 , C07D277/56 , C07D303/24 , C07C321/00
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves reacting cysteine (or a salt or an ester thereof) and an aryl carboxylic acid to form a thiazoline ring, stereospecifically alkylating the thiazoline ring, and hydrolyzing the thiazoline ring to obtain a 2-alkylcysteine (or related compound). The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.
摘要翻译：非天然氨基酸例如2-烷基化氨基酸允许合成更多种类的肽和非肽类药物活性剂。制备2-烷基氨基酸的方法包括使半胱氨酸（或其盐或其酯）和芳基羧酸反应形成噻唑啉环，立体特异性烷基化噻唑啉环，并水解噻唑啉环以获得2-烷基半胱氨酸（或相关化合物）。本发明还公开了一种制备与脱铁硫杆菌相关的一类铁螯合剂的方法，所述铁螯合剂全部含有噻唑啉环。在该方法中，芳基腈或亚氨酸酯与半胱氨酸，2-烷基半胱氨酸或半胱氨酸酯缩合。

7. 发明申请

US20030236435A1 Synthesis of 2-alkylcysteine via substituted thiazoline ester 有权
标题翻译：通过取代噻唑啉酯合成2-烷基半胱氨酸
公开(公告)号：US20030236435A1
公开(公告)日：2003-12-25
申请号：US10439282
申请日：2003-05-15
申请人： Genzyme Corporation
发明人： Rayomand H. Gimi , Mukund S. Chorghade , Sunil V. Mhaskar
IPC分类号： C07C323/52
CPC分类号： C07C227/18 , C07B2200/07 , C07C229/36 , C07C255/53 , C07C255/54 , C07C257/08 , C07C319/02 , C07C319/06 , C07C319/12 , C07C319/20 , C07D277/12 , C07D303/24 , C07C323/58
摘要： Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. In one embodiment, the present invention relates to a method of preparing a 2-alkylcysteine comprising condensing cysteine with an aryl nitrile to form a 2-arylthiazoline-4-carboxylic acid, esterifying the 2-arylthiazoline-4-carboxylic acid using a substituted or unsubstituted alcohol group comprising one or more chiral carbons, and alkylating at the 4-position of the thiazoline ring to form a 2-aryl-4-alkyl-thiazoline-4-carboxylic acid ester. The chiral templates present in the thiazoline carboxylic acid ester can provide face selectivity, and consequently desired stereochemistry, during the delivery of an alkyl group to the 4-position of the thiazoline ring. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In one embodiment, an aryl nitrile is condensed with cysteine or a 2-alkyl cysteine.
摘要翻译：非天然氨基酸例如2-烷基化氨基酸允许合成更多种类的肽和非肽类药物活性剂。在一个实施方案中，本发明涉及制备2-烷基半胱氨酸的方法，其包括将半胱氨酸与芳基腈缩合以形成2-芳基噻唑啉-4-羧酸，使用取代或取代的2-芳基噻唑啉-4-羧酸酯化2-芳基噻唑啉-4-羧酸包含一个或多个手性碳的未取代的醇基，在噻唑啉环的4-位烷基化，形成2-芳基-4-烷基 - 噻唑啉-4-羧酸酯。存在于噻唑啉羧酸酯中的手性模板可以在将烷基递送至噻唑啉环的4-位期间提供面选择性，并因此提供所需的立体化学。本发明还公开了一种制备与脱铁硫杆菌相关的一类铁螯合剂的方法，所述铁螯合剂全部含有噻唑啉环。在一个实施方案中，芳基腈与半胱氨酸或2-烷基半胱氨酸缩合。

8. 发明授权

US5869067A Bi-aromatic compounds and pharmaceutical and cosmetic compositions 失效
标题翻译：双芳族化合物和药物和化妆品组合物
公开(公告)号：US5869067A
公开(公告)日：1999-02-09
申请号：US311790
申请日：1994-09-26
申请人： Jean-Phillippe Rocher , Jean-Michel Bernardon
发明人： Jean-Phillippe Rocher , Jean-Michel Bernardon
IPC分类号： A61K31/136 , A61K31/137 , A61K31/166 , A61K31/195 , A61K31/196 , A61K31/245 , C07C251/24 , C07C257/08 , C07C257/18 , C07C327/58 , A61K9/00 , A61K31/04 , A61K31/045 , A61K31/085 , A61K31/095 , A61K31/33
CPC分类号： A61K31/136 , A61K31/137 , A61K31/166 , A61K31/195 , A61K31/196 , A61K31/245 , C07C251/24 , C07C257/08 , C07C257/18 , C07C327/58 , C07C2102/10 , C07C2103/74
摘要： The present invention relates to new aromatic compounds, to their preparation and to their use in human and veterinary medicine and in cosmetic compositions.
摘要翻译：本发明涉及新的芳族化合物，其制备方法及其在人和兽医学和化妆品组合物中的用途。

9. 发明授权

US4987135A Substituted benzene derivatives, processes for their production and antitumor compositions containing them 失效
标题翻译：取代苯衍生物，其制备方法和含有它们的抗肿瘤组合物
公开(公告)号：US4987135A
公开(公告)日：1991-01-22
申请号：US324559
申请日：1989-03-16
申请人： Takahiro Haga , Nobutoshi Yamada , Hideo Sugi , Toru Koyanagi , Hiroshi Okada
发明人： Takahiro Haga , Nobutoshi Yamada , Hideo Sugi , Toru Koyanagi , Hiroshi Okada
IPC分类号： C07D295/12 , A61K31/50 , A61K31/505 , A61P35/00 , C07C257/08 , C07C275/54 , C07C313/34 , C07C323/44 , C07C327/58 , C07C329/04 , C07C381/04 , C07C381/08 , C07D213/64 , C07D213/81 , C07D237/14 , C07D239/34 , C07D295/155 , C07D401/12 , C07F9/24 , C07F9/6512
CPC分类号： C07D213/64 , C07C257/08 , C07C327/58 , C07D237/14 , C07D239/34 , C07D295/155 , C07D401/12 , C07F9/65127 , C07C2101/08 , C07C2101/14
摘要： A substituted benzene derivative represented by a formula: ##STR1## where A represents: ##STR2## wherein X is a hydrogen atom, a halogen atom or a nitro group, R.sup.1 is --X.sup.1 Z.sup.1 (X.sup.1 is an oxygen atom or a sulfur atom and Z.sup.1 is a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group, a substituted or unsubstituted aryl group or a substituted or unsubstituted heteroaryl group), --COZ.sup.1 group (Z.sup.1 is as defined above), ##STR3## group (Z.sup.1 is as defined above, Z.sup.2 is --CO.sub.2 Z.sup.3 wherein Z.sup.3 is the same as Z.sup.1, or --SO.sub.2 Z.sup.3 wherein Z.sup.3 is as defined above and n is 0 or 1), ##STR4## (Z.sup.1 and Z.sup.3 are as defined above) or ##STR5## (X.sup.2, X.sup.3 and X.sup.4 are, respectively, an oxygen atom or a sulfur atom and Z.sup.4 and Z.sup.5 are the same as Z.sup.1), and R.sup.3 is a nitro group or ##STR6## (R.sup.4 and R.sup.5 are, respectively, an alkyl group, or they may form a heterocyclic group together with the adjacent nitrogen atom), or ##STR7## wherein X and R.sup.3 are as defined above and R.sup.2 is --X.sup.1 Z.sup.1 (X.sup.1 and Z.sup.1 are as defined above); Y is a halogen atom, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkylthio group, a nitro group or ##STR8## (R.sup.6 and R.sup.7 are, respectively, a substituted or unsubstituted alkyl group); R is ##STR9## (R.sup.8 is the same as Y and q is an integer of 1 to 4), ##STR10## (R.sup.8 is as defined above, and r is an integer of 1 to 3) or ##STR11## (R.sup.8 and r are defined above); and m is an integer, of 1 to 4, or its salt.

10. 发明授权

US4492657A Imines of alkyl 4-halomethylbenzoates 失效
标题翻译：亚胺的4-卤代甲基苯甲酸烷基酯
公开(公告)号：US4492657A
公开(公告)日：1985-01-08
申请号：US488126
申请日：1983-04-25
申请人： Lorenz Heiss
发明人： Lorenz Heiss
IPC分类号： C07C257/08 , C07C67/00 , C07C241/00 , C07C119/20
CPC分类号： C07C257/08
摘要： New alkyl (4-halomethyl)iminobenzoates of the formula ##STR1## and their HCl or HBr salts, R denoting C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -alkoxyethyl and X denoting Cl or Br. These compounds are prepared by reaction of p-cyanobenzyl chloride or p-cyanobenzyl bromide with a C.sub.1 -C.sub.4 -alcohol or C.sub.1 -C.sub.4 -alkoxyethanol in the presence of hydrogen chloride or bromide. The new imines serve as intermediate products, inter alia for the preparation of optical brighteners of the bisbenzoxazolylstilbene class.
摘要翻译：式（IMAGE）的新的烷基（4-卤甲基）亚氨基苯甲酸酯及其HCl或HBr盐，R表示C 1 -C 4烷基或C 1 -C 4 - 烷氧基乙基，X表示Cl或Br。这些化合物是通过在氯化氢或溴化氢存在下使对氰基苄基氯或对氰基苄基溴与C 1 -C 4醇或C 1 -C 4 - 烷氧基乙醇反应来制备的。新的亚胺作为中间体产品，尤其用于制备双苯并恶唑基茋类荧光增白剂。

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