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1. 发明申请

US20030199712A1 Process for the preparation of cephalosporin intermediate and its use for the manufacture of cephalosporin compounds 失效
标题翻译：头孢菌素中间体的制备方法及其用于制造头孢菌素的化合物
公开(公告)号：US20030199712A1
公开(公告)日：2003-10-23
申请号：US10245490
申请日：2002-09-18
申请人： Orchid Chemicals and Pharmaceuticals Limited
发明人： Pandurang Balwant Deshpande , Parven Kumar Luthra , Pratik Ramesh Sathe , Sivakumaran Sundaravadivelan , Praveen Nagesh Ganesh
IPC分类号： C07C249/12
CPC分类号： C07F9/14 , C07C249/12 , C07C251/38 , C07C251/60 , C07D501/00 , C07F9/091
摘要： The present invention relates to a process for the preparation of 4-halogeno-2-substitutedimino-3-oxo-butyric acid of formula (I) 1 wherein R1 represents CH3, CRaRbCOORc where Ra and Rb independently represent hydrogen or methyl and Rc represents hydrogen or (C1-C6)alkyl, X represents halogen such as chlorine or bromine, also discloses the activation of this acid and its further use in the preparation of cephalosporanic antibiotics (II) in excellent yields and purity
摘要翻译：本发明涉及一种制备式（I）的4-卤代-2-取代亚氨基-3-氧代 - 丁酸的方法，其中R 1表示CH 3，CR a R COOR c， a>和R b独立地表示氢或甲基，R c表示氢或（C 1 -C 6）烷基，X表示卤素如氯或溴，也公开了该酸的活化及其在制备中的其它用途的头孢菌素抗生素（II）的产率和纯度优良

2. 发明申请

US20040082560A1 Process for the preparation of cefixime 失效
标题翻译：头孢克肟的制备方法
公开(公告)号：US20040082560A1
公开(公告)日：2004-04-29
申请号：US10310177
申请日：2002-12-05
申请人： ORCHID CHEMICALS AND PHARMACEUTICALS LIMITED
发明人： Pandurang Balwant Deshpande , Gautam Kumar Das , Pramod Narayan Deshpande , Ramasubbu Chandrasekaran , Padmanabhan Ramar , John Muthiah Raja Jeyakumar
IPC分类号： A61K031/545 , C07D501/14
CPC分类号： C07D501/00
摘要： The present invention provides an improved process for the preparation of cefixime of formula (I), with an improved quality having/possessing better color and solubility.
摘要翻译：本发明提供了制备式（I）的头孢克肟的改进方法，其具有/具有更好的颜色和溶解度的改进的质量。

3. 发明申请

US20030232983A1 Process for preparation of penam derivatives from cepham derivatives 失效
标题翻译：头孢烯衍生物的制备方法
公开(公告)号：US20030232983A1
公开(公告)日：2003-12-18
申请号：US10309201
申请日：2002-12-04
申请人： Orchid Chemicals and Pharmaceuticals Limited
发明人： Pandurang Balwant Deshpande , Senthil Kumar Udayampalayam Palanisamy , Gnanaprakasam Andrew
IPC分类号： C07D499/44
CPC分类号： C07D499/00 , Y02P20/55
摘要： The present invention relates to a process for preparing 2null-methyl-2null-substituted methyl penam derivatives from cepham derivatives, more particularly the present invention provides a novel process for preparing 2null-heterocyclyl methyl penam derivatives of the formula (I) 1 wherein R1 represents carboxylic acid protecting group; R2 and R3 may be same or different and independently represent hydrogen, halogen, NH2, acylamino, phthalimido with a proviso that both R2 and R3 are not NH2, acylamino, phthalimido; Het represents a 5 or 6 membered nitrogen containing heterocycle ring system having one or more heteroatoms selected from O, S, or N.
摘要翻译：本发明涉及一种由头孢烯衍生物制备2α-甲基-2β-取代的甲基对苯二甲酸衍生物的方法，更具体地说，本发明提供了制备式（I）的2ba-杂环基甲基半阴离子衍生物的新方法，其中R 1表示羧基酸保护基; R2和R3可以相同或不同，并且独立地代表氢，卤素，NH2，酰氨基，苯二甲酰亚氨基，条件是R2和R3都不是NH2，酰氨基，邻苯二甲酰亚氨基; Het表示具有一个或多个选自O，S或N的杂原子的5或6元含氮杂环体系。

4. 发明申请

US20040002600A1 Process for the conversion of penam ring system to cepham ring system 审中-公开
标题翻译：将Penam环系统转换为cepham环系统的过程
公开(公告)号：US20040002600A1
公开(公告)日：2004-01-01
申请号：US10207110
申请日：2002-07-30
申请人： Orchid Chemicals and Pharmaceuticals Limited
发明人： Pandurang Balwant Deshpande , Senthilkumar Udayampalayam Palanisamy , Padmanabhan Ramar
IPC分类号： C07D501/02 , C07D501/10
CPC分类号： C07D417/12 , C07D499/00 , C07D501/00
摘要： The present invention relates to a new process for the preparation of cephalosporin derivative of formula (I) 1 wherein R1 represents p-methoxybenzyl, p-nitrobenzyl, o-chlorobenzyl or diphenylmethyl; R2 represents CH3 or CRaRbCOORc where Ra and Rb independently represent hydrogen or methyl and Rc represents hydrogen or (C1-C6) alkyl; R3 represents hydrogen, acyl, phenacyl, formyl or trityl group.
摘要翻译：本发明涉及制备式（I）的头孢菌素衍生物的新方法，其中R1表示对甲氧基苄基，对硝基苄基，邻氯苄基或二苯基甲基; R 2表示CH 3或CR a R c COOR c，其中R 1和R 2独立地表示氢或甲基，R c表示氢或（C 1 -C 6）烷基; R3表示氢，酰基，苯甲酰甲酰基，甲酰基或三苯甲基。

5. 发明申请

US20030130502A1 Synthesis of ceftiofur intermediate 失效
标题翻译：头孢噻呋中间体的合成
公开(公告)号：US20030130502A1
公开(公告)日：2003-07-10
申请号：US10208879
申请日：2002-08-01
申请人： Orchid Chemicals and Pharmaceuticals Limited
发明人： Pramod Narayan Deshpande , Bhausaheb Pandharinath Khadangale , Surulichamy Senthil Kumar , Gautam Kumar Das
IPC分类号： C07D501/14
CPC分类号： C07D501/00
摘要： The present invention relates to a process for preparation of 7-amino-3-null2-(furylcarbonyl)thiomethylnull-3-cephem-4-carboxylic acid (I) by the condensation of 7-aminocephalosporanic acid (II) with furyl-2-carbonylthiol (III) in the presence of borontrifluoride or its complex, in an organic solvent or mixture of solvents at 0-50null C.
摘要翻译：本发明涉及7-氨基-3- [2-（呋喃基羰基）硫代甲基] -3-头孢烯-4-羧酸（I）的制备方法，其通过7-氨基头孢烷酸（II）与呋喃基 - 在三氟化硼或其配合物的存在下，在有机溶剂或溶剂混合物中，在0-50℃下加入2-羰基硫醇（III）

6. 发明授权

US08828999B2 Pyrimidine compounds and their uses 有权
标题翻译：嘧啶化合物及其用途
公开(公告)号：US08828999B2
公开(公告)日：2014-09-09
申请号：US13777813
申请日：2013-02-26
申请人： Orchid Chemicals and Pharmaceuticals Limited
发明人： Ganapavarapu Sharma , Venkatesan Parameswaran , Gopalan Balasubramanian , Santosh Vishwakarma , Sanjeev Saxena
IPC分类号： A61K31/535 , C07D401/04 , C07D239/42 , C07D265/28 , A61K31/5377
CPC分类号： C07D239/42 , A61K31/5377 , C07D265/28 , C07D401/04
摘要： Pyrimidine compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof, are useful are useful as PDE4 inhibitors and are useful for treating PDE4 mediated diseases and in the treatment of immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; atherosclerosis; cancer; cachexia; ischemic-induced cell damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; ARDS; psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; asthma; COPD; bone resorption diseases; multiple sclerosis; sepsis; septic shock; toxic shock syndrome and fever.
摘要翻译：通式（I）的嘧啶化合物，其衍生物，类似物，互变异构形式，立体异构体，多晶型物，水合物，溶剂合物，药学上可接受的盐，药物组合物，代谢物和前药可用作PDE4抑制剂，并且可用于治疗 PDE4介导的疾病和治疗免疫疾病，炎症，疼痛障碍，类风湿关节炎; 骨质疏松症多发性骨髓瘤葡萄膜炎急性和慢性粒细胞白血病; 动脉粥样硬化癌症; 恶病质缺血诱导的细胞损伤; 胰腺β细胞破坏; 骨关节炎类风湿性脊柱炎; 痛风性关节炎炎症性肠病; ARDS; 银屑病; 克罗恩病; 过敏性鼻炎; 溃疡性结肠炎过敏反应接触性皮炎; 肌肉退化; 哮喘; COPD; 骨吸收疾病; 多发性硬化症败血症败血性休克中毒性休克综合征和发烧。

7. 发明申请

US20040015020A1 Method for the conversion of a Z-isomer into E-isomer 失效
标题翻译：将Z-异构体转化为E-异构体的方法
公开(公告)号：US20040015020A1
公开(公告)日：2004-01-22
申请号：US10310048
申请日：2002-12-05
申请人： ORCHID CHEMICALS AND PHARMACEUTICALS LIMITED
发明人： Pandurang Balwant Deshpande , Senthil Kumar Udayampalayam Palanisamy , Gnanaprakasam Andrew
IPC分类号： C07C041/32
CPC分类号： C07C37/055 , C07B2200/09 , C07C41/32 , C07C43/215 , C07C39/21
摘要： A method of converting (Z)-1-(3,5-disubstituted phenyl)-2-(4-substituted phenyl)ethene of general formula (II) to (E)-1-(3,5-disubstituted phenyl)-2-(4-substituted phenyl)ethene of general formula (I) 1 wherein R1, R2 and R3 are same or different and independently represent (C1-C4)alkyl, (C1-C4)alkoxy(C1-C4)alkyl, (C1-C4)alkoxy(C1-C4)alkoxy(C1-C4)alkyl, allyl, vinyl, silyl, formyl, acyl, aryl(C1-C4)alkyl or substituted aryl(C1-C4)alkyl group. The present invention also provides a process for the conversion of (E)-1-(3,5-disubstituted phenyl)-2-(4-substituted phenyl)ethene of general formula (I) prepared by a process described above to E-resveratrol of the formula (III). 2
摘要翻译：将通式（II）的（Z）-1-（3,5-二取代苯基）-2-（4-取代苯基）乙烯转化成（E）-1-（3,5-二取代苯基） - 通式（I）的2-（4-取代苯基）乙烯，其中R 1，R 2和R 3相同或不同并且独立地表示（C 1 -C 4）烷基，（C 1 -C 4）烷氧基（C 1 -C 4） -C 1-4）烷氧基（C 1 -C 4）烷氧基（C 1 -C 4）烷基，烯丙基，乙烯基，甲硅烷基，甲酰基，酰基，芳基（C 1 -C 4）烷基或取代的芳基（C 1 -C 4）本发明还提供了通过上述方法制备的通式（I）的（E）-1-（3,5-二取代苯基）-2-（4-取代苯基）乙烯转化为E- 式（III）的白藜芦醇。

8. 发明申请

US20030216567A1 New method for the preparation of ceftiofur sodium and its intermediates 失效
标题翻译：制备头孢噻呋钠及其中间体的新方法
公开(公告)号：US20030216567A1
公开(公告)日：2003-11-20
申请号：US10207103
申请日：2002-07-30
申请人： ORCHID CHEMICALS AND PHARMACEUTICALS LIMITED
发明人： Pandurang Balwant Deshpande , Praven Kumar Luthra , Pratik Ramesh Sathe , Sivakumaran Sundaravadivelan , Praveen Nagesh Ganesh
IPC分类号： C07D501/14
CPC分类号： C07D501/00
摘要： The present invention relates to a new method for the preparation of Ceftiofur acid of formula (I), 1 its pharmaceutically acceptable salt such as sodium or hydrochloride and also provides two new intermediates of formulae (V) and (VI) 2 wherein X represents halogen atom such as chlorine or bromine and R represents p-methoxybenzyl, p-nitrobenzyl or diphenylmethyl group.
摘要翻译：本发明涉及一种制备式（I）的头孢噻呋及其药学上可接受的盐如钠或盐酸盐的新方法，并且还提供了两种新的式（Ⅴ）和（Ⅵ）中间体，其中X代表卤素原子作为氯或溴，R代表对甲氧基苄基，对硝基苄基或二苯基甲基。

9. 发明申请

US20130172350A1 PYRIMIDINE COMPOUNDS AND THEIR USES 有权
标题翻译：吡嗪化合物及其用途
公开(公告)号：US20130172350A1
公开(公告)日：2013-07-04
申请号：US13777813
申请日：2013-02-26
申请人： Orchid Chemicals and Pharmaceuticals Limited
发明人： Ganapavarapu SHARMA , Venkatesan Parameswaran , Gopalan Balasubramanian , Santosh Vishwakarma , Sanjeev Saxena
IPC分类号： C07D239/42
CPC分类号： C07D239/42 , A61K31/5377 , C07D265/28 , C07D401/04
摘要： Pyrimidine compounds of the general formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof, are useful are useful as PDE4 inhibitors and are useful for treating PDE4 mediated diseases and in the treatment of immunological diseases, inflammation, pain disorder, rheumatoid arthritis; osteoporosis; multiple myeloma; uveititis; acute and chronic myelogenous leukemia; atherosclerosis; cancer; cachexia; ischemic-induced cell damage; pancreatic beta cell destruction; osteoarthritis; rheumatoid spondylitis; gouty arthritis; inflammatory bowel disease; ARDS; psoriasis; Crohn's disease; allergic rhinitis; ulcerative colitis; anaphylaxis; contact dermatitis; muscle degeneration; asthma; COPD; bone resorption diseases; multiple sclerosis; sepsis; septic shock; toxic shock syndrome and fever.
摘要翻译：通式（I）的嘧啶化合物，其衍生物，类似物，互变异构形式，立体异构体，多晶型物，水合物，溶剂合物，药学上可接受的盐，药物组合物，代谢物和前药可用作PDE4抑制剂，并且可用于治疗 PDE4介导的疾病和治疗免疫疾病，炎症，疼痛障碍，类风湿关节炎; 骨质疏松症多发性骨髓瘤葡萄膜炎急性和慢性粒细胞白血病; 动脉粥样硬化癌症; 恶病质缺血诱导的细胞损伤; 胰腺β细胞破坏; 骨关节炎类风湿性脊柱炎; 痛风性关节炎炎症性肠病; ARDS; 银屑病; 克罗恩病; 过敏性鼻炎; 溃疡性结肠炎过敏反应接触性皮炎; 肌肉退化; 哮喘; COPD; 骨吸收疾病; 多发性硬化症败血症败血性休克中毒性休克综合征和发烧。

10. 发明申请

WO2011098938A1 NOVEL SOLVATE OF DEXLANSOPRAZOLE 审中-公开
标题翻译：新戊酰唑啉的新溶剂
公开(公告)号：WO2011098938A1
公开(公告)日：2011-08-18
申请号：PCT/IB2011/050488
申请日：2011-02-04
申请人： ORCHID CHEMICALS AND PHARMACEUTICALS LIMITED , REGURI, Buchi Reddy , UPPARAPALLI, Sampath kumar , KUNCHITHAPATHAM, Thirumurugan , NATARAJAN, Sabarinathan , SAMBASHIVAM, Thiyagarajan , MUNUSWAMY, Suresh , SWAMINATHAN, Susi
发明人： REGURI, Buchi Reddy , UPPARAPALLI, Sampath kumar , KUNCHITHAPATHAM, Thirumurugan , NATARAJAN, Sabarinathan , SAMBASHIVAM, Thiyagarajan , MUNUSWAMY, Suresh , SWAMINATHAN, Susi
IPC分类号： C07D401/12 , A61K31/4439 , C07D235/28 , A61K31/415 , A61P1/00 , A61K31/44 , A61P1/04
CPC分类号： C07D401/12 , C07D235/28
摘要： The present invention provides novel solvate of dexlansoprazole (or R- lansoprazole), particularly diol solvate and its hydrate form of dexlansoprazole (or R-lansoprazole) which is chemically known as (R)-2-[[[3-methyl-4-(2,2,2- trifluoroethoxy)-2-pyridinyl] methyl] sulfmyl]-lH-benzimidazole compound of the formula (I), as well as processes for the preparation thereof. The said solvates are useful in the preparation of dexlansoprazole with enhanced chiral purity and better HPLC purity with less sulphone impurity content.
摘要翻译：本发明提供了右旋兰索唑（或R-兰索拉唑）特别是二醇溶剂合物及其水合物形式的右兰索拉唑（或R-兰索拉唑）的新型溶剂合物，其化学上称为（R）-2 - [[[3-甲基-4- （2,2,2-三氟乙氧基）-2-吡啶基]甲基]亚磺酰基] -1H-苯并咪唑化合物及其制备方法。所述溶剂合物可用于制备具有增强的手性纯度的右兰索拉唑和更好的HPLC纯度，较少的砜含量。

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