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1. 发明授权

US07041830B2 Process for preparing (RS) 3-methyl-1-(2-piperidinyl phenyl) butyl amine 失效
标题翻译：制备（RS）3-甲基-1-（2-哌啶基苯基）丁胺的方法
公开(公告)号：US07041830B2
公开(公告)日：2006-05-09
申请号：US10404007
申请日：2003-03-31
申请人： Uttam Ramrao Kalkote , Mukund Keshao Gurjar , Shreerang Vidyadhar Joshi , Suresh Mahadev Kadam , Harish Kashinath Mondkar
发明人： Uttam Ramrao Kalkote , Mukund Keshao Gurjar , Shreerang Vidyadhar Joshi , Suresh Mahadev Kadam , Harish Kashinath Mondkar
IPC分类号： C07D211/26
CPC分类号： C07D295/135
摘要： The Present invention relates to a process for the preparation of (RS) 3-methyl-1-(2-piperidinyl phenyl) butyl amine of formula 1. (RS) 3-Methyl-1-(2-piperidinyl phenyl butyl amine having formula 1 is an important key intermediate for the synthesis of repaglinide of formula 2 an oral hypoglycemic agent.
摘要翻译：本发明涉及制备式（1）的（RS）3-甲基-1-（2-哌啶基苯基）丁基胺的方法。（RS）3-甲基-1-（2-哌啶基苯基丁基胺，其具有式 1是口服降血糖药合成式2瑞格列奈的重要关键中间体。

2. 发明授权

US06504044B2 Process for the preparation of 1-[cyano(aryl)methyl] cyclohexanol 有权
标题翻译： 1- [氰基（芳基）甲基]环己醇的制备方法
公开(公告)号：US06504044B2
公开(公告)日：2003-01-07
申请号：US09796084
申请日：2001-02-28
申请人： Subhash Prataprao Chavan , Subhash Krishnaji Kamat , Latha Sivadasan , Kamalam Balakrishnan , Dushant Anandrao Khobragade , Ravindranathan Thottapillil , Mukund Keshao Gurjar , Uttam Ramrao Kalkote
发明人： Subhash Prataprao Chavan , Subhash Krishnaji Kamat , Latha Sivadasan , Kamalam Balakrishnan , Dushant Anandrao Khobragade , Ravindranathan Thottapillil , Mukund Keshao Gurjar , Uttam Ramrao Kalkote
IPC分类号： C07C25500
CPC分类号： C07C253/30 , C07C2601/08 , C07C2601/14 , C07C255/36 , C07C255/37
摘要： A process for the preparation of 1-[(cyano) aryl methyl] cyclohexanol of the general formula 1 (1a-d) by reacting cyclohexanone with the carbanions of an aryl acetonitrile of the general formula 3 (3a-d), a) R1=H, R2=H b) R1=OMe R2=H c) R1=OMe R2=OMe d) R1=OMe R2=cyclopentyloxy using a base, isolating the compound of formula 1 and purifying the compound of formula 1a-d by crystallisation is disclosed.
摘要翻译：通过使环己酮与通式3（3a-d）的芳基乙腈的碳阴离子反应制备通式1（1a-d）的1 - [（氰基）芳基甲基]环己醇的方法，a）R1 公开了通过结晶分离式1化合物和纯化式1a-d的化合物的方法，其中R 1 = OMe R 2 = OMc）R 1 = OMe R 2 =使用碱的环戊氧基。

3. 发明授权

US06350912B1 One pot process for the preparation of 1-[2-dimethylamino-(4-methoxyphenyl)-ethyl]cyclohexanol 有权
标题翻译：用于制备1- [2-二甲基氨基 - （4-甲氧基苯基） - 乙基]环己醇的一锅法
公开(公告)号：US06350912B1
公开(公告)日：2002-02-26
申请号：US09796082
申请日：2001-02-28
申请人： Subhash Prataprao Chavan , Subhash Krishnaji Kamat , Latha Sivadasan , Kamalam Balakrishnan , Dushant Anandrao Khobragade , Ravindranathan Thottapillil , Mukund Keshao Gurjar , Uttam Ramrao Kalkote
发明人： Subhash Prataprao Chavan , Subhash Krishnaji Kamat , Latha Sivadasan , Kamalam Balakrishnan , Dushant Anandrao Khobragade , Ravindranathan Thottapillil , Mukund Keshao Gurjar , Uttam Ramrao Kalkote
IPC分类号： C07C21100
CPC分类号： C07C217/74 , C07C213/02 , C07C2601/14
摘要： A process for the preparation of 2-[dimethylamino-(4-methoxyphenyl)ethyl]-cyclohexanol of formula 1 by reducing 1-[cyano(4-methoxyphenyl)-methyl]cyclohexanol of formula 2 with a formylating agent in a protic solvent in the presence of a catalyst, removing the catalyst by filtration, isolating and purifying the compound of formula 1 is disclosed.
摘要翻译：通过用甲酰化剂将式2的1- [氰基（4-甲氧基苯基） - 甲基]环己醇在质子性溶剂中还原，制备式1的2- [二甲基氨基 - （4-甲氧基苯基）乙基] - 环己醇的方法公开了催化剂的存在，通过过滤除去催化剂，分离和纯化式1的化合物。

4. 发明授权

US06713639B1 Process for preparing enantiomerically pure (S)-3-hydroxy-gamma-butyrolactone 失效
标题翻译：制备对映体纯（S）-3-羟基-γ-丁内酯的方法
公开(公告)号：US06713639B1
公开(公告)日：2004-03-30
申请号：US10281615
申请日：2002-10-28
申请人： Mukund Keshao Gurjar , Pradeep Kumar , Anis Naim Deshmukh , Rajesh Kumar Upadhyay , Puspesh Kumar Upadhyay
发明人： Mukund Keshao Gurjar , Pradeep Kumar , Anis Naim Deshmukh , Rajesh Kumar Upadhyay , Puspesh Kumar Upadhyay
IPC分类号： C07D30720
CPC分类号： C07D307/33
摘要： The present invention relates to a process for the in situ preparation of optically pure (S)-3,4-dihydroxybutyric acid derivatives represented by the Formula [2] and more particularly, to a process which enables preparing optically pure (S)-3-hydroxy-&ggr;-butyrolactone represented by Formula [1] by oxidation of &agr;- or &bgr;-(1,4) linked disaccharide or oligosaccharide with an oxidant under basic condition to give acid and cyclization sequentially under acidic condition to give (S)-3-hydroxy-&ggr;-butyrolactone.
摘要翻译：本发明涉及一种原位制备由式[2]表示的光学纯的（S）-3,4-二羟基丁酸衍生物的方法，更具体地说，涉及能够制备光学纯的（S）-3 通过在碱性条件下用氧化剂氧化α-或β-（1,4）连接的二糖或寡糖，由式[1]表示的 - 羟基-γ-丁内酯在酸性条件下依次酸化和环化，得到（S） - 3-羟基-γ-丁内酯。

5. 发明授权

US06541647B2 Methods of synthesis of substituted tetrahydrofuran compound 有权
标题翻译：合成取代四氢呋喃化合物的方法
公开(公告)号：US06541647B2
公开(公告)日：2003-04-01
申请号：US09969799
申请日：2001-10-02
申请人： Mukund Shankar Chorghade , Mukund Keshao Gurjar , Palakodety Radha Krishna , Sista Venkata Sai Lalitha , Kashinath Sadalapure , Susanta Sekhar Adhikari , Andappan Murugaiah Subbaiah Murugaiah , Sunil Vyankatesh Mhaskar , Gangavaram Vasantha Madhava Sharma , Tangallapally Rajendra Prasad , Punna Sreenivas , Vavilala Goverdhan Reddy , Aminul Islam , Chittineni Hari Prasad , Alla Venkata Rama Rao
发明人： Mukund Shankar Chorghade , Mukund Keshao Gurjar , Palakodety Radha Krishna , Sista Venkata Sai Lalitha , Kashinath Sadalapure , Susanta Sekhar Adhikari , Andappan Murugaiah Subbaiah Murugaiah , Sunil Vyankatesh Mhaskar , Gangavaram Vasantha Madhava Sharma , Tangallapally Rajendra Prasad , Punna Sreenivas , Vavilala Goverdhan Reddy , Aminul Islam , Chittineni Hari Prasad , Alla Venkata Rama Rao
IPC分类号： C07D30733
CPC分类号： C07D307/14 , C07D307/12 , C07D307/32
摘要： The invention includes inter alia new methods for preparation of the pharmaceutically active compound 2-(4-fluorophenoxymethyl)-5-(4-N-hydroxyureidyl-1 -butynyl)-tetrahydrofuran and precursors thereof.
摘要翻译：本发明尤其包括制备药学活性化合物2-（4-氟苯氧基甲基）-5-（4-N-羟基脲基-1-丁炔基） - 四氢呋喃及其前体的新方法。

6. 发明申请

US20090247545A1 SUBSTITUTED OXAZOLIDINONE DERIVATIVES 审中-公开
标题翻译：取代的氧杂环丁酮衍生物
公开(公告)号：US20090247545A1
公开(公告)日：2009-10-01
申请号：US11577083
申请日：2004-12-28
申请人： Mukund Keshao Gurjar , Madhusudan Nagorao Deshmukh , Anita Mehta , Sudershan Kumar Arora , Ashok Rattan
发明人： Mukund Keshao Gurjar , Madhusudan Nagorao Deshmukh , Anita Mehta , Sudershan Kumar Arora , Ashok Rattan
IPC分类号： A61K31/496 , C07D413/10 , A61P31/04
CPC分类号： C07D263/20 , C07D413/10
摘要： The present invention provides substituted oxazolidinone derivatives, which can be used as antimicrobial agents. Compounds disclosed can be used for the treatment or prevention of a condition caused by or contributed to by bacteria, such as, inter alia, multiply-resistant Staphylococci, Streptococci, Enterococci, Bacterioides spp., Clostridium spp., Mycobacterium spp. Bacillus spp., Corynebacterium spp. Heptoslreptacoccus spp. Listeria spp., Legionella spp., Haemophilus influenza, Moraxella, Eschericia faecalis, and Eschericia coli. Processes for the preparation of disclosed compounds, pharmaceutical compositions thereof, and method of treating microbial infection are provided.
摘要翻译：本发明提供了可用作抗微生物剂的取代的恶唑烷酮衍生物。所公开的化合物可用于治疗或预防由细菌引起的或由细菌引起的病症，例如多重耐药葡萄球菌，链球菌，肠球菌，细菌属，梭菌属，分枝杆菌属。芽孢杆菌属，棒状杆菌属肝细胞线粒体利斯特氏菌属（Listeria spp。），军团菌属（Legionella spp。），嗜血杆菌流感，流感嗜血杆菌，大肠埃希氏菌和大肠埃希氏菌。提供了制备所公开化合物的方法，其药物组合物，以及治疗微生物感染的方法。

7. 发明授权

US06310221B1 Methods for synthesis of substituted tetrahydrofuran compound 有权
标题翻译：合成取代四氢呋喃化合物的方法
公开(公告)号：US06310221B1
公开(公告)日：2001-10-30
申请号：US09347087
申请日：1999-07-02
申请人： Mukund Shankar Chorghade , Mukund Keshao Gurjar , Palakodety Radha Krishna , Sista Venkata Sai Lalitha , Kashinath Sadalapure , Susanta Sekhar Adhikari , Andappan Murugaiah Subbaiah Murugaiah , Sunil Vyankatesh Mhaskar , Gangavaram Vasantha Madhava Sharma , Tangallapally Rajendra Prasad , Punna Sreenivas , Vavilala Goverdhan Reddy , Aminul Islam , Chittineni Hari Prasad , Alla Venkata Rama Rao
发明人： Mukund Shankar Chorghade , Mukund Keshao Gurjar , Palakodety Radha Krishna , Sista Venkata Sai Lalitha , Kashinath Sadalapure , Susanta Sekhar Adhikari , Andappan Murugaiah Subbaiah Murugaiah , Sunil Vyankatesh Mhaskar , Gangavaram Vasantha Madhava Sharma , Tangallapally Rajendra Prasad , Punna Sreenivas , Vavilala Goverdhan Reddy , Aminul Islam , Chittineni Hari Prasad , Alla Venkata Rama Rao
IPC分类号： C07D30512
CPC分类号： C07D307/14 , C07D307/12 , C07D307/32
摘要： The invention includes inter alia new methods for preparation of the pharmaceutically active compound 2-(4-fluorophenoxymethyl)-5-(4-N-hydroxyureidyl-1-butynyl)-tetrahydrofuran and precursors thereof.
摘要翻译：本发明尤其包括制备药学活性化合物2-（4-氟苯氧基甲基）-5-（4-N-羟基脲基-1-丁炔基） - 四氢呋喃及其前体的新方法。

8. 发明授权

US06191279B1 Dipyrano-quinolinones useful as anti viral agents and a process for preparing the same 有权
标题翻译：可用作抗病毒剂的二亚氨基 - 喹啉酮及其制备方法
公开(公告)号：US06191279B1
公开(公告)日：2001-02-20
申请号：US09321851
申请日：1999-05-28
申请人： Mukund Keshao Gurjar , Gangavaram Vasantha Madhava Sharma , Aindivelu Ilangovan , Ven Narayanan
发明人： Mukund Keshao Gurjar , Gangavaram Vasantha Madhava Sharma , Aindivelu Ilangovan , Ven Narayanan
IPC分类号： C07D49112
CPC分类号： C07D491/14 , A61K31/436 , Y10S436/815
摘要： The invention relates to novel dipyrano-quinolinone class of compounds having the general formula: Wherein R is hydrogen, alkyl optionally substituted about C-1 to C-10 alkenyl optionally substituted about C-1 to C-10 with one or more double bounds, alkynyl optionally substituted about C-1 to C-10 with one or more triple bonds, aryl, hetero aryl, carbocyclic aryl, alkyl aryl, alcyclic compounds, C-1 to C-6 alkyl with terminal dialkyl amino group, thio alkyl, hydroxyl alkyl groups; R1 is H, lower dialkyl amino alkyls such as methyl, ethyl, propyl, and other alkyl groups or b-amino acid moieties, hydroxy alkyl groups having optionally substituted about C-1 to C-10 carbons, acid amides such as aliphatic acids, aromatic acids, sulphonic acids trihalo acids. x—x is either a carbon-carbon single bond or a carbon-carbon double bond; R2 and R3, R4 and R5 are each independently hydrogen and methyl there by resulting the cis and trans diastereomers as well as enantiomers; R4 and R5 are each independently hydrogen and methyl while R6 and R7 are each independently hydrogen and hydroxyl/—OR8, where R8 is independently alkyl, aryl alkyl, amino alkyl, hydroxy alkyl with C-1 to C-10 carbons, sugars which include mono saccharides both in the furanose form as well as pyranose form, amino sugars, disaccharides, amino acids, small peptides through lower alkyl spacer groups, thereby resulting the cis and trans diastereomers as well as enantiomers; and a process for producing the above novel dipyrano-quinolinone class of compounds.
摘要翻译：本发明涉及具有以下通式的新颖的二吡喹烷 - 喹啉酮类化合物：其中R是氢，任选取代有C1-至C-10烯基的烷基，该C 1至C 10链烯基具有一个或多个双重界限的C-1至C-10，芳基，杂芳基，碳环芳基，烷基芳基，异环化合物，具有末端二烷基氨基的C 1至C 6烷基，硫代烷基，羟基，C 1 -C 6烷基，烷基; R 1为H，低级二烷基氨基烷基如甲基，乙基，丙基和其它烷基或b-氨基酸部分，具有任选取代为C-1至C-10碳原子的羟基烷基，酰胺如脂肪酸，芳香酸，磺酸三卤酸.xx是碳 - 碳单键或碳 - 碳双键; R2和R3，R4和R5各自独立地为氢和甲基，得到顺式和反式非对映异构体以及对映体; R4和R5各自独立氢和甲基，而R6和R7各自独立地为氢和羟基-OR8，其中R8独立地是烷基，芳基烷基，氨基烷基，具有C-1至C-10碳的羟基烷基，包括单糖的糖，呋喃糖形式以及吡喃糖形式，氨基糖，二糖，氨基酸，通过低级烷基间隔基团的小肽，从而得到顺式和反式非对映体以及对映异构体; 以及制备上述新型双吡喃 - 喹啉酮类化合物的方法。

9. 发明授权

US07109353B2 Process for preparing 5,6-dihydro-4-(S)-(ethylamino)-6-(S) methyl-4H-thieno[2,3b]thiopyran-2-sulphonamide-7,7-dioxide HCl 有权
标题翻译：制备5,6-二氢-4-（S） - （乙基氨基）-6-（S）甲基-4H-噻吩并[2,3-b]噻喃-2-磺酰胺-7,7-二氯化氢的方法
公开(公告)号：US07109353B2
公开(公告)日：2006-09-19
申请号：US11024029
申请日：2004-12-28
申请人： Mukund Keshao Gurjar , Madhusudan Nagorao Deshmukh , Vincent Paul , Venkatasubramaniam Radhakrishnan Tarur , Dhananjay Govind Sathe , Santosh Pratap Pardeshi , Sanjay Janardhan Naik , Tushar Anil Naik
发明人： Mukund Keshao Gurjar , Madhusudan Nagorao Deshmukh , Vincent Paul , Venkatasubramaniam Radhakrishnan Tarur , Dhananjay Govind Sathe , Santosh Pratap Pardeshi , Sanjay Janardhan Naik , Tushar Anil Naik
IPC分类号： C07D335/04
CPC分类号： C07D495/04
摘要： The present invention relates to an improved process for the preparation of 5,6-dihydro-4-(S)-(ethylamino)-6-(S)methyl-4H-thieno[2,3b]thiopyran-2-sulphonamide-7,7-dioxide hydrochloride of formula (I) commonly known as Dorzolamide Hydrochloride useful as an agent to reduce intraoccular pressure by inhibiting carbonic anhydrase enzyme
摘要翻译：本发明涉及制备5,6-二氢-4-（S） - （乙基氨基）-6-（S）甲基-4H-噻吩并[2,3-b]噻喃-2-磺酰胺-7 通常称为多佐胺酰盐酸盐的式（I）的二氧化二盐酸盐可用作通过抑制碳酸酐酶来降低脑内压的药剂

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