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1. 发明申请

WO2013011460A1 PROCESS FOR THE PREPARATION AND PURIFICATION OF AN INTERMEDIATE FOR FONDAPARINUX SODIUM 审中-公开
标题翻译： FONDAPARINUX SODIUM中间体的制备和纯化方法
公开(公告)号：WO2013011460A1
公开(公告)日：2013-01-24
申请号：PCT/IB2012/053651
申请日：2012-07-17
申请人： RANBAXY LABORATORIES LIMITED , NAGARAJU, P. , THAKUR, Mandeep , PANDYA, Bhargav
发明人： NAGARAJU, P. , THAKUR, Mandeep , PANDYA, Bhargav
IPC分类号： C07H1/06 , C07H3/10
CPC分类号： C07H1/06 , C07H3/10
摘要： The present invention relates to process for the preparation and purification of 4- O -β-D-glucopyranosyl-1,6-anhydro-β-D-glucopyranose represented by Formula (II). The process of the invention can be used in the production of fondaparinux sodium, a heparin and blood clotting factor Xa inhibitor.
摘要翻译：本发明涉及制备和纯化由式（II）表示的4-O-β-D-吡喃葡萄糖基-1,6-脱水-β-D-吡喃葡萄糖的方法。本发明的方法可用于磺达肝素钠，肝素和凝血因子Xa抑制剂的生产。

2. 发明申请

WO2013011459A1 PROCESS FOR THE PREPARATION OF FONDAPARINUX 审中-公开
标题翻译： FONDAPARINUX的制备方法
公开(公告)号：WO2013011459A1
公开(公告)日：2013-01-24
申请号：PCT/IB2012/053649
申请日：2012-07-17
申请人： RANBAXY LABORATORIES LIMITED , PANDYA, Bhargav , NAGARAJU, P.
发明人： PANDYA, Bhargav , NAGARAJU, P.
IPC分类号： C07H7/033
CPC分类号： C07H7/033
摘要： The present invention relates to process for preparation of O-(2,3-Di-O-benzyl- β -D-glucopyranuronicacid)-(1→4)-3-O-acetyl-1,6-anhydro-2-azido-2-deoxy- β -D-glucopyranose represented by Formula (II) comprising oxidation of O-(2,3-Di-O-benzyl- β -D-glucopyranosyl)-(1→4)-3-O-acetyl-1,6-anhydro-2-azido-2-deoxy- β -D-glucopyranose represented by Formula (I) with N-bromosuccinamide (NBS), bisacetoxy iodobenzene (iodobenzene diacetate) or mixture thereof, optionally in presence of 2,2,6,6-tetramethylpiperidine-1-oxyl (hereinafter referred as TEMPO). The process of the invention are useful for the production of fondaparinux sodium, a heparin and blood clotting factor Xa inhibitor.
摘要翻译：本发明涉及制备O-（2,3-二-O-苄基-β-D-吡喃葡萄糖醛酸） - （1→4）-3-O-乙酰基-1,6-脱水-2-叠氮基由式（II）表示的包含O-（2,3-二-O-苄基-β-D-吡喃葡萄糖基） - （1→4）-3-O-乙酰基的氧化的2-脱氧-β-D-吡喃葡萄糖由式（I）代表的具有N-溴代琥珀酰胺（NBS），双乙酰氧基碘苯（二乙酸碘苯）或其混合物的-1,6-脱水-2-叠氮基-2-脱氧-β-D-吡喃葡萄糖， 2,6,6-四甲基哌啶-1-氧基（以下称TEMPO）。本发明的方法可用于生产磺达肝素钠，肝素和凝血因子Xa抑制剂。

3. 发明申请

WO2006035293A1 POLYMORPHIC FORMS OF QUETIAPINE HEMIFUMARATE 审中-公开
标题翻译：高效液相色谱的多态性
公开(公告)号：WO2006035293A1
公开(公告)日：2006-04-06
申请号：PCT/IB2005/002860
申请日：2005-09-27
申请人： RANBAXY LABORATORIES LIMITED , PANDYA, Bhargav , ARYAN, Ram, Chander , KUMAR, Yatendra
发明人： PANDYA, Bhargav , ARYAN, Ram, Chander , KUMAR, Yatendra
IPC分类号： C07D281/16
CPC分类号： C07D281/16
摘要： The present invention relates to novel polymorphic forms of quetiapine hemifumarate, process for their preparation and pharmaceutical compositions thereof.
摘要翻译：本发明涉及喹硫平半富马酸盐的新型多晶型物，其制备方法及其药物组合物。

4. 发明申请

WO2006040643A3 POLYMORPHIC FORMS OF EFAVIRENZ AND PROCESSES FOR THEIR PREPARATION 审中-公开
公开(公告)号：WO2006040643A3
公开(公告)日：2006-04-20
申请号：PCT/IB2005/003013
申请日：2005-10-10
申请人： RANBAXY LABORATORIES LIMITED , SHARMA, Ramnik , BHUSHAN, Kumar, Hari , ARYAN, Ram, Chander , SINGH, Nitu , PANDYA, Bhargav , KUMAR, Yatendra
发明人： SHARMA, Ramnik , BHUSHAN, Kumar, Hari , ARYAN, Ram, Chander , SINGH, Nitu , PANDYA, Bhargav , KUMAR, Yatendra
IPC分类号： C07D265/18 , A61K31/535 , A61P31/18
摘要： The present invention relates to novel polymorphic forms of efavirenz. The novel polymorphic forms are designated as Forms α, β, γ, γ1, γ2, ω,δ, N, O and P of efavirenz. The present invention further relates to amorphous form of efavirenz. The invention also relates to the processes for their preparation and use in pharmaceutical compositions useful in the treatmentof HIV-1 infection.

5. 发明申请

WO2013011442A1 PROCESS FOR PREPARATION OF FONDAPARINUX AND ITS INTERMEDIATES 审中-公开
标题翻译： FONDAPARINUX及其中间体的制备方法
公开(公告)号：WO2013011442A1
公开(公告)日：2013-01-24
申请号：PCT/IB2012/053610
申请日：2012-07-13
申请人： RANBAXY LABORATORIES LIMITED , PANDYA, Bhargav , SURADKAR, Swapnil , PATHADE, Ajinath
发明人： PANDYA, Bhargav , SURADKAR, Swapnil , PATHADE, Ajinath
IPC分类号： C07D493/04
CPC分类号： C07D493/04
摘要： The present invention relates to a process for the preparation of 3-O-benzyl- 1,2-O- isopropylidene-α-D-glucofuranuronic acid (Formula IV) and ester (Formula V) thereof. The process comprises benzylation of l,2:5,6-di-O-isopropylidene-α-D-glucofuranose (Formula I; hereinafter, referred to as diacetone-D-glucose) in the presence of tetrabutylammonium bromide, followed by selective hydrolysis of the product formed (Formula II) using sulfuric acid to obtain 3-O-benzyl- 1,2-O-isopropylidene-α-D- glucofuranose (Formula III). Compound of Formula III is then oxidized to compound of Formula IV which upon esterification provides corresponding ester of Formula V. The process of the invention can be used in the production of fondaparinux sodium, a heparin and blood clotting factor Xa inhibitor.(Formula I, II, III, IV, V) (I) (II) (III) (IV) (V) wherein R is optionally branched alkyl group.
摘要翻译：本发明涉及制备3-O-苄基-1,2-二-O-异亚丙基-α-D-吡喃葡萄糖醛酸（式IV）及其酯（式V）的方法。该方法包括在四丁基溴化铵存在下苄基化1,2：5,6-二-O-异亚丙基-d-呋喃葡糖（式I;以下称为双丙酮-D-葡萄糖），然后选择性水解使用硫酸形成（式II）的产物，得到3-O-苄基-1,2-（2-异亚丙基-α-D-呋喃并呋喃糖）（式III）。然后将式III的化合物氧化成式IV的化合物，其在酯化时提供相应的式V的酯。本发明的方法可用于磺达肝素钠，肝素和凝血因子Xa抑制剂的生产（式I， II，III，IV，V）（I）（II）（III）（Ⅳ）（Ⅴ）其中R是任意支链的烷基。

6. 发明申请

WO2006040645A1 N-(3,5-DICHLOROPYRIDIN-4-YL)-2,4,5-ALKOXY AND 2,3,4-ALKOXY BENZAMIDE DERIVATIVES AS PDE-IV (PHOPHODIESTERASE TYPE-IV) INHIBITORS FOR THE TREATMENT OF INFLAMMATORY DISEASES SUCH AS ASTHMA 审中-公开
标题翻译：作为治疗炎症性疾病的PDE-IV（PHOPHODIESTERASE TY-IV）抑制剂的N-（3,5-二氯吡啶-4-基）-2,4,5-烷氧基和2,3,4-烷氧基苯甲酰胺衍生物哮喘
公开(公告)号：WO2006040645A1
公开(公告)日：2006-04-20
申请号：PCT/IB2005/003017
申请日：2005-10-11
申请人： RANBAXY LABORATORIES LIMITED , SHARMA, Ramnik , BHUSHAN, Kumar, Hari , PANDYA, Bhargav , ARYAN, Ram, Chander , KUMAR, Yatendra
发明人： SHARMA, Ramnik , BHUSHAN, Kumar, Hari , PANDYA, Bhargav , ARYAN, Ram, Chander , KUMAR, Yatendra
IPC分类号： C07D213/75 , C07C235/56 , A61P11/06
CPC分类号： C07D213/75 , C07D213/89
摘要： The present invention relates to benzamide derivatives, which can be used as selective inhibitors of phosphodiesterase (PDE) type IV, having the structure of Formula (I), its pharmaceutically acceptable salts, pharmaceutically acceptable solvates, enantiomers, diastereomers of N-oxides wherein R1 is hydrogen, alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heteroaryl, heterocyclyl, aralkyl, heterocyclylalkyl, heteroarylalkyl or cycloalkylalkyl; R2 is aryl, heteroaryl, heterocyclyl of cycloalkyl; and R3 is alkyl, alkenyl, alkynyl, aryl, cycloalkyl, heteroaryl, heterocyclyl, aralkyl, heterocyclylalkyl, heteroarylalkyl or cycloalkylalkyl. Compounds disclosed herein can be useful in the treatment of inflammatory diseases, AIDS, asthma, arthritis, bronchitis, chronic obstructer pulmonary disease (COPD), psoriasis, allergic rhinitis, shock, atopic dermatitis, Crohn’ s disease, adult respiratory distress syndrome (ARDS), eosinophilic granuloma, allergic conjunctivitis, osteoarthritis and ulcerative colitis.
摘要翻译：本发明涉及苯甲酰胺衍生物，其可用作IV型磷酸二酯酶（PDE）的选择性抑制剂，其具有式（I）的结构，其药学上可接受的盐，药学上可接受的溶剂合物，对映异构体，N-氧化物的非对映异构体，其中R1 烷基，烯基，炔基，芳基，环烷基，杂芳基，杂环基，芳烷基，杂环基烷基，杂芳基烷基或环烷基烷基; R2是芳基，杂芳基，环烷基的杂环基; R 3为烷基，烯基，炔基，芳基，环烷基，杂芳基，杂环基，芳烷基，杂环基烷基，杂芳基烷基或环烷基烷基。本文公开的化合物可用于治疗炎性疾病，AIDS，哮喘，关节炎，支气管炎，慢性阻塞性肺疾病（COPD），牛皮癣，过敏性鼻炎，休克，特应性皮炎，克罗恩病，成人呼吸窘迫综合征（ARDS ），嗜酸性肉芽肿，过敏性结膜炎，骨关节炎和溃疡性结肠炎。

7. 发明申请

WO2006018807A1 CRYSTALLINE FORMS OF CEFDINIR 审中-公开
标题翻译： CEFDINIR的晶体形式
公开(公告)号：WO2006018807A1
公开(公告)日：2006-02-23
申请号：PCT/IB2005/052691
申请日：2005-08-15
申请人： RANBAXY LABORATORIES LIMITED , MAHENDRU, Manu , ARYAN, Ram, Chander , KUMAR, Satish , PANDYA, Bhargav , DUGGAL, Sanjam , GADE, Sanjay , KUMAR, Yatendra
发明人： MAHENDRU, Manu , ARYAN, Ram, Chander , KUMAR, Satish , PANDYA, Bhargav , DUGGAL, Sanjam , GADE, Sanjay , KUMAR, Yatendra
IPC分类号： C07D501/00 , A61K31/546 , A61P31/04
CPC分类号： C07D501/00
摘要： The invention relates to processes for the preparation of crystalline polymorphic forms of cefdinir of formula (I). More particularly, it relates to the preparation of crystalline polymorphic forms of cefdinir designated as Forms B and C. The invention also relates to pharmaceutical compositions that include the polymorphic forms B and C, and the use of the compositions for treating bacterial infections.
摘要翻译：本发明涉及制备式（I）的头孢地尼的结晶多晶形式的方法。更具体地说，本发明涉及被称为形式B和C的头孢地尼的晶体多晶形式的制备。本发明还涉及包含多晶型B和C的药物组合物，以及该组合物用于治疗细菌感染的用途。

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