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公开(公告)号：US20220411463A1
公开(公告)日：2022-12-29
申请号：US17432929
申请日：2019-04-07
申请人： Khashayar KARIMIAN
发明人： Khashayar KARIMIAN , Javad MOKHTARI , Amir Hassan ZARNANI , Aliakbar MOOSAVI-MOVAHEDI , Maryam NOURISEFAT , Bita ZAMIRI , Leila FOTOUHI
IPC分类号： C07K1/14 , C07K16/06 , C07K14/765 , C12N15/10
摘要： Biological small molecules, proteins or nucleic acids (target molecules, TM) are isolated in from biological media such as blood serum, cytoplasm, nucleoplasm etc. by a novel process (mate and separate) involving the use of PEGylated recognition molecule (PEG-RM) with high specificity and binding for TM, affording a macromolecular complex PEG-RM.TM, from which the target protein can be obtained in pure form.
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2.发明授权
公开(公告)号：US5914401A
公开(公告)日：1999-06-22
申请号：US37982
申请日：1998-03-11
申请人： Ian Egle , Regis C.S.H. Leung-Toung , Bo Lei , Tim Fat Tam , Tao Xin , Khashayar Karimian
发明人： Ian Egle , Regis C.S.H. Leung-Toung , Bo Lei , Tim Fat Tam , Tao Xin , Khashayar Karimian
IPC分类号： C07D215/22 , C07D215/233 , C07D215/56 , C07D401/00 , C07D215/16 , C07D265/34
CPC分类号： C07D215/233 , C07D215/56
摘要： Novel process for the preparation of quinolone carboxylic acid derivatives of general formula I, and intermediates thereof as illustrated in Scheme 1 wherein the key intermediate is a compound of formula IX. ##STR1##
摘要翻译： 用于制备通式I的喹诺酮羧酸衍生物的新方法及其中间体，如方案1所示，其中关键中间体是式IX的化合物。
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公开(公告)号：US5596093A
公开(公告)日：1997-01-21
申请号：US469506
申请日：1995-06-06
摘要： A process from preparing 5-halogenated 2,3-O-cyclocytidine derivatives comprising reacting 2,3-O-cyclocytidine with a halogenating reagent, preferably N-bromosuccinimide, in the presence of an acid such as acetic or trifluoroacetic.
摘要翻译： 制备5-卤代2,3-O-环胞苷衍生物的方法，包括在酸如乙酸或三氟乙酸存在下，使2,3-碘 - 环胞苷与卤化试剂，优选N-溴代琥珀酰亚胺反应。
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公开(公告)号：US5527782A
公开(公告)日：1996-06-18
申请号：US191192
申请日：1994-02-02
摘要： A 5'-halo-2,3'-O-cyclocytidine of Formula I: ##STR1## wherein: X is a bromide, chloride, or iodide;Y is halide, sulfate, acetate, tosyl, mesyl, benzoate, and phosphate;R.sup.1 is hydrogen; andR.sup.2 is a hydroxy protecting group.Pharmaceutical compositions containing the above compounds exhibit antineoplastic activity.
摘要翻译： 式I的5'-卤-2,3'-O-环胞苷：其中：X是溴，氯或碘; Y是卤化物，硫酸盐，乙酸盐，甲苯磺酰，甲磺酰，苯甲酸盐和磷酸盐; R1是氢; R2为羟基保护基。 含有上述化合物的药物组合物表现出抗肿瘤活性。
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5.发明授权Azithromycin monohydrate isopropanol clathrate and methods for the manufacture thereof 有权阿奇霉素一水合物异丙醇包合物及其制备方法公开(公告)号：US06245903B1
公开(公告)日：2001-06-12
申请号：US09373549
申请日：1999-08-13
IPC分类号： C07H1708
CPC分类号： C07H17/08
摘要： A novel form of azithromycin and processes for preparation of pure azithromycin monohydrate isopropanol clathrate (3 molecules of isopropanol for every 10 molecules of azithromycin monohydrate) has been obtained. Preparation of the novel form of azithromycin comprises the steps of dissolving azithromycin in isopropanol, followed by the slow addition of water to the organic solution.
摘要翻译： 已经获得了阿奇霉素的新型形式和用于制备纯阿齐霉素一水合物异丙醇包合物（每10分子阿奇霉素一水合物的3分子异丙醇）的方法。 阿奇霉素的新形式的制备包括将阿奇霉素溶解在异丙醇中，然后缓慢加入有机溶液中的步骤。
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6.发明授权Thiadiazole compounds useful as inhibitors of cysteine activity dependent enzymes 失效可用作半胱氨酸活性依赖性酶抑制剂的噻二唑化合物
公开(公告)号：US6162791A
公开(公告)日：2000-12-19
申请号：US33937
申请日：1998-03-02
IPC分类号： A61K31/433 , A61K38/00 , A61P17/10 , A61P19/02 , A61P31/00 , A61P43/00 , C07D285/08 , C07D417/06 , C07K5/06 , C07K5/062 , C07K5/065 , A61K31/41 , C07D285/68
CPC分类号： C07D285/08 , C07K5/06034 , C07K5/06043
摘要： Novel 1,2,4-thiadiazole compounds are provided, which are effective as inhibitors of cysteine activity-dependent enzymes and in particular of cysteine proteases. The compounds are useful in treating acne by inhibition of transglutaminase, common cold by inhibition of human rhinovirus 3C protease and inflammatory joint disease by inhibition of cathepsins. The compounds of the present invention are 3,5-disubstituted 1,2,4-thiadazole of the general formula (I): ##STR1## where Z is a nitrogen containing group with recognition sequence for the enzyme and Y is a substituent that tunes the reactivity of the inhibitor towards the thiol group of the cysteine activity-dependent enzyme. The Y group may also serve in recognition.
摘要翻译： 提供新的1,2,4-噻二唑化合物，其作为半胱氨酸活性依赖性酶，特别是半胱氨酸蛋白酶的抑制剂是有效的。 这些化合物可用于通过抑制转谷氨酰胺酶来治疗痤疮，通过抑制组织蛋白酶抑制人类鼻病毒3C蛋白酶和炎症性关节疾病，常见感冒。 本发明的化合物是通式（I）的3,5-二取代的1,2,4-噻唑：其中Z是具有酶识别序列的含氮基团，Y是调节反应性的取代基 半胱氨酸活性依赖性酶的巯基的抑制剂。 Y团队也可以承认。
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7.发明授权Methods of making ureas and guanidines including, terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates therefor 失效制造脲类和胍类的方法包括特拉唑嗪，哌唑嗪，多沙唑嗪，替加沙星，三甲氧唑嗪，喹唑啉和布氮唑啉（2-取代喹唑啉化合物的示例），和美巴汀及其中间体
公开(公告)号：US6080860A
公开(公告)日：2000-06-27
申请号：US939414
申请日：1997-09-29
申请人： Khashayar Karimian , Keshava Murthy , Darren Hall
发明人： Khashayar Karimian , Keshava Murthy , Darren Hall
IPC分类号： C07D271/10 , C07D271/113 , C07D295/215 , C07D307/24 , C07D319/20 , C07D405/12 , C07D413/12 , C07C275/70 , C07D241/04 , C07D407/04
CPC分类号： C07D271/113 , C07D295/215 , C07D307/24 , C07D319/20 , C07D405/12 , C07D413/10 , C07D413/12
摘要： Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediates suitable for use in such methods of synthesis are taught.
摘要翻译： 教导了合成包括特拉唑嗪，哌唑嗪，多沙唑嗪，替沙星，替马唑星，喹喔啉和布那唑辛（2-氨基取代的喹唑啉的示例性），Meobentine和Bethanidine的取代脲类和胍类的新方法，以及适用于这些合成方法的新型中间体 。
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8.发明授权Methods of making ureas and guanidines, including terazosin, prazosin, doxazosin, tiodazosin, trimazosin, quinazosin, and bunazosin (exemplary of 2-substituted quinazoline compounds), and meobentine, and bethanidine and intermediates thereof 失效制造脲类和胍类的方法，包括特拉唑嗪，哌唑嗪，多沙唑嗪，替沙星，三甲氧唑嗪，喹唑啉和布氮唑嗪（2-取代喹唑啉化合物的示例）和meobentine以及其中间体
公开(公告)号：US5686612A
公开(公告)日：1997-11-11
申请号：US453093
申请日：1995-05-30
申请人： Khashayar Karimian , Keshava Murthy , Darren Hall
发明人： Khashayar Karimian , Keshava Murthy , Darren Hall
IPC分类号： C07D271/10 , C07D271/113 , C07D295/215 , C07D307/24 , C07D319/20 , C07D405/12 , C07D413/12 , C07D403/02 , C07D403/06
CPC分类号： C07D271/113 , C07D295/215 , C07D307/24 , C07D319/20 , C07D405/12 , C07D413/10 , C07D413/12
摘要： Novel methods for the synthesis of substituted ureas and guanidines including Terazosin, Prazosin, Doxazosin, Tiodazosin, Trimazosin, Quinasin and Bunazosin (exemplary of 2-amino substituted Quinazolines), Meobentine and Bethanidine and novel intermediates suitable for use in such methods of synthesis are taught.
摘要翻译： 教导了合成包括特拉唑嗪，哌唑嗪，多沙唑嗪，替沙星，替马唑星，喹喔啉和布那唑辛（2-氨基取代的喹唑啉的示例性），Meobentine和Bethanidine的取代脲类和胍类的新方法，以及适用于这些合成方法的新型中间体 。
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公开(公告)号：US5519129A
公开(公告)日：1996-05-21
申请号：US326854
申请日：1994-10-21
IPC分类号： C07H19/06 , C07H19/073 , C07C279/02
CPC分类号： C07H19/06
摘要： A composition of a 1:1 molar complex of guanidine and 3'-azido-3'-deoxythymidine (AZT) which is generated at about pH above 9 and disrupted by pH below about 9. This complex is a useful intermediate in the purification of AZT.
摘要翻译： 胍和3'-叠氮基-3'-脱氧胸苷（AZT）的1:1摩尔配合物的组合物，其在约pH大于9时产生并且通过pH低于约9被破坏。该复合物是纯化中的有用中间体 AZT。
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公开(公告)号：US20190211150A1
公开(公告)日：2019-07-11
申请号：US16326924
申请日：2017-08-22
申请人： Khashayar KARIMIAN
IPC分类号： C08G65/323 , C08G65/332 , C08G65/333 , C07C227/34
CPC分类号： C08G65/323 , C07B2200/07 , C07C227/34 , C07C301/00 , C08G65/329 , C08G65/3326 , C08G65/33396 , C07C229/36
摘要： The present invention is related to a product for the resolution of racemic mixtures in which various separation processes of a salt composed of a PEGylated resolving agent and an enantiomer in a racemic mixture is utilized. Separation can be caused by temperature-dependent phase transformation of the said salt pair in aqueous or organic media as well as other methods used is separation of PEG such as salting out (e.g. addition of ammonium sulfate). The first cycle of racemic resolution by this method was shown to afford 85% optically pure amino acid from a 50:50 mixture of racemic L,D-amino acids esters. An additional cycle improved optical purity up to 95%.
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