公开(公告)号：WO2008032099A3

公开(公告)日：2008-03-20

申请号：PCT/GB2007/003510

申请日：2007-09-14

Applicant: CIPLA LIMITED ,  CURTIS, Philip, Anthony ,  PATHI, Srinivas, Laxminarayan ,  KANKAN, Rajendra, Narayanrao ,  RAO, Dharmaraj, Ramachandra ,  PHULL, Manjinder, Singh

Inventor： PATHI, Srinivas, Laxminarayan ,  KANKAN, Rajendra, Narayanrao ,  RAO, Dharmaraj, Ramachandra ,  PHULL, Manjinder, Singh

IPC: C07D215/18 ,  A61K31/47

Abstract: The invention relates to processes for making montelukast of formula I and to intermediates for use in the process, in particular compounds of formulas 2 - 7:

公开(公告)号：WO2007077443A1

公开(公告)日：2007-07-12

申请号：PCT/GB2007/000009

申请日：2007-01-03

Applicant: CIPLA LIMITED ,  CURTIS, Philip, Anthony ,  PATHI, Srinivas, Laxminarayan ,  ACHARYA, Vinod ,  RAO, Dharmaraj, Ramachandra ,  KANKAN, Rajendra, Narayanrao

Inventor： PATHI, Srinivas, Laxminarayan ,  ACHARYA, Vinod ,  RAO, Dharmaraj, Ramachandra ,  KANKAN, Rajendra, Narayanrao

IPC: C07D211/32 ,  C07D491/10

CPC classification number: C07D211/32 ,  C07D491/10

Abstract: The invention relates to new compounds of formula (III): wherein R is a C 1 -C 4 linear or branched alkyl group. The invention also relates to new compounds of formula (IV) wherein M is a metal. The invention also relates to methods of making compounds of formulas (III) and (IV) and to methods of making donepezil and pharmaceutically acceptable salts thereof, such as donepezil hydrochloride, using the compounds.

Abstract translation: 本发明涉及新的式（III）化合物：其中R是C 1 -C 4直链或支链烷基。 本发明还涉及新的式（IV）化合物，其中M是金属。 本发明还涉及制备式（III）和（IV）化合物的方法以及使用该化合物制备多奈哌齐及其药学上可接受的盐如盐酸多奈哌齐的方法。

公开(公告)号：WO2010097583A1

公开(公告)日：2010-09-02

申请号：PCT/GB2010/000333

申请日：2010-02-24

Applicant: CIPLA LIMITED ,  RAO, Dharmaraj, Ramachandra ,  PATHI, Srinivas, Laxminarayan ,  KANKAN, Rajendra, Narayanrao ,  CURTIS, Philip, Anthony

Inventor： RAO, Dharmaraj, Ramachandra ,  PATHI, Srinivas, Laxminarayan ,  KANKAN, Rajendra, Narayanrao ,  CURTIS, Philip, Anthony

IPC: C07D401/12 ,  A61K31/4439 ,  A61P1/04

CPC classification number: C07D401/12

Abstract: The present invention provides a polymorph of esomeprazole potassium termed "Form C", which is in the form of an ethanol solvate. There is also provided processes for preparing Form C of esomeprazole potassium and pharmaceutical compositions comprising it.

Abstract translation: 本发明提供了称为“形式C”的埃索美拉唑钾的多晶型物，其为乙醇溶剂化物的形式。 还提供了用于制备埃索美拉唑钾的形式C的方法和包含它的药物组合物。

公开(公告)号：WO2008043996A2

公开(公告)日：2008-04-17

申请号：PCT/GB2007003821

申请日：2007-10-09

Applicant: CIPLA LTD ,  CURTIS PHILIP ANTHONY ,  PATHI SRINIVAS LAXMINARAYAN ,  PUPPALA RAVIKUMAR ,  KANKAN RAJENDRA NARAYANRAO ,  RAO DHARMARAJ RAMACHANDRA

Inventor： PATHI SRINIVAS LAXMINARAYAN ,  PUPPALA RAVIKUMAR ,  KANKAN RAJENDRA NARAYANRAO ,  RAO DHARMARAJ RAMACHANDRA

IPC: C07D405/14

CPC classification number: C07D405/14

Abstract: A process for the preparation of trityl olmesartan comprising (a) condensing 4-(1-hydroxy- 1-methylethyl)-2-propyl-imidazol-5-carboxylic acid alkyl ester with trityl biphenyl bromide in the presence of a polar aprotic solvent and a base selected from the group consisting of alkali metal carbonates, alkali metal hydroxides, alkali metal alkoxides, and tertiary amines to obtain a compound of formula (V): b) deesterifying the compound of formula (V) with a base; and c) reacting the product of step (b) with 4-halomethyl-5-methyl-2-oxo-1,3-dioxolene of formula (IV): wherein X is halogen selected from F or Cl or Br or I, to obtain trityl olmesartan medoxomil of formula. The trityl olmesartan medoxomil may be deprotected to produce olmesartan medoxomil.

Abstract translation: 一种制备三苯甲基奥美沙坦的方法，包括（a）在极性非质子溶剂存在下将4-（1-羟基-1-甲基乙基）-2-丙基 - 咪唑-5-羧酸烷基酯与三苯甲基联苯溴烷缩合，和 选自碱金属碳酸盐，碱金属氢氧化物，碱金属醇盐和叔胺的碱，得到式（Ⅴ）化合物：b）使式（Ⅴ）化合物与碱脱酯反应; 和c）使步骤（b）的产物与式（IV）的4-卤代甲基-5-甲基-2-氧代-1,3-二氧杂环戊烯反应：其中X是选自F或Cl或Br或I的卤素， 获得配方的三美质奥美沙坦酯。 三苯甲基奥美沙坦酯可以去保护以产生奥美沙坦酯。

公开(公告)号：WO2008032099A2

公开(公告)日：2008-03-20

申请号：PCT/GB2007003510

申请日：2007-09-14

Applicant: CIPLA LTD ,  CURTIS PHILIP ANTHONY ,  PATHI SRINIVAS LAXMINARAYAN ,  KANKAN RAJENDRA NARAYANRAO ,  RAO DHARMARAJ RAMACHANDRA ,  PHULL MANJINDER SINGH

Inventor： PATHI SRINIVAS LAXMINARAYAN ,  KANKAN RAJENDRA NARAYANRAO ,  RAO DHARMARAJ RAMACHANDRA ,  PHULL MANJINDER SINGH

IPC: C07D215/18 ,  A61K31/47

CPC classification number: C07D215/18

Abstract: The invention relates to processes for making montelukast and to intermediates for use in the process, in particular compounds of formulas 2-7: L=OAc, OTs, OTf5OMs; where X=Cl, Br, I.

Abstract translation: 本发明涉及制备孟鲁司特和用于该方法的中间体的方法，特别是式2-7的化合物：L = OAc，OTs，OTf5OMs; 其中X = Cl，Br，I.

公开(公告)号：WO2008125867A2

公开(公告)日：2008-10-23

申请号：PCT/GB2008001343

申请日：2008-04-16

Applicant: CIPLA LTD ,  CURTIS PHILIP ANTHONY ,  RAO DHARMARAJ RAMACHANDRA ,  KANKAN RAJENDRA NARAYANRAO ,  PATHI SRINIVAS LAXMINARAYAN

Inventor： RAO DHARMARAJ RAMACHANDRA ,  KANKAN RAJENDRA NARAYANRAO ,  PATHI SRINIVAS LAXMINARAYAN

IPC: C07C205/44 ,  C07D239/94

CPC classification number: C07C205/44 ,  C07C51/285 ,  C07C201/08 ,  C07C201/12 ,  C07C205/59 ,  C07C227/12 ,  C07D239/88 ,  C07C229/56 ,  C07C65/21

Abstract: There is provided a compound of formula (III), and a process for preparing a compound of formula (V) comprising converting a compound of formula (III) to the compound (V), wherein (X) is fluoro, chloro, bromo or iodo. There is also provided a process for preparing a compound of formula (Xl) comprising converting a compound of formula (X) to the compound (Xl). The compounds (V) and (Xl) so prepared may be used in a process for preparing gefitinib.

Abstract translation: 提供式（III）化合物和制备式（V）化合物的方法，包括将式（III）化合物转化为化合物（V），其中（X）为氟，氯，溴或 碘。 还提供了制备式（XI）化合物的方法，其包括将式（X）化合物转化成化合物（XI）。 如此制备的化合物（V）和（XI）可以用于制备吉非替尼的方法中。

公开(公告)号：WO2008102145A2

公开(公告)日：2008-08-28

申请号：PCT/GB2008/000602

申请日：2008-02-21

Applicant: CIPLA LIMITED ,  CURTIS, Philip, Anthony ,  RAO, Dharmaraj, Ramachandra ,  KANKAN, Rajendra, Narayanrao ,  PATHI, Srinivas, Laxminarayan ,  BANGALORE, Gopalakrishna, Sumana

Inventor： RAO, Dharmaraj, Ramachandra ,  KANKAN, Rajendra, Narayanrao ,  PATHI, Srinivas, Laxminarayan ,  BANGALORE, Gopalakrishna, Sumana

IPC: C07D401/12 ,  A61K31/4427 ,  A61P1/04

CPC classification number: C07D417/12 ,  C07D401/12

Abstract: A process for preparing Form A of (S)-5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)- methyl]sulfinyl]-1 H-benzimidazole magnesium dihydrate, processes for preparing various intermediates useful in the preparation of Form A of (S)-5-methoxy-2-[[(4-methoxy-3,5- dimethyl-2-pyridinyl)-methyl]sulfinyl]-1 H-benzimidazole magnesium dihydrate and a novel polymorphic Form II of 5-methoxy-2-[[(4-methoxy-3,5-dimethyl-2-pyridinyl)-methyl]thio]-1 H- benzimidazole.

Abstract translation: 制备（S）-5-甲氧基-2 - [[（4-甲氧基-3,5-二甲基-2-吡啶基） - 甲基]亚磺酰基] -1H-苯并咪唑镁二水合物的形式A的方法， 可用于制备（S）-5-甲氧基-2 - [[（4-甲氧基-3,5-二甲基-2-吡啶基） - 甲基]亚磺酰基] -1H-苯并咪唑镁二水合物形式A的各种中间体和 5-甲氧基-2 - [[（4-甲氧基-3,5-二甲基-2-吡啶基） - 甲基]硫基] -1H-苯并咪唑的新型多晶型II。

公开(公告)号：WO2006117802A2

公开(公告)日：2006-11-09

申请号：PCT/IN2006/000077

申请日：2006-02-21

Applicant: CIPLA LIMITED ,  PATHI, Srinivas, Laxminarayan ,  KANKAN, Rajendra, Narayanrao ,  RAO, Dharmaraj, Ramachandra

Inventor： PATHI, Srinivas, Laxminarayan ,  KANKAN, Rajendra, Narayanrao ,  RAO, Dharmaraj, Ramachandra

IPC: C07D401/12

CPC classification number: C07D401/12

Abstract: A process for preparation of rabeprazole sodium comprising oxidation of wet or dry rabeprazole sulphide with sodium hypohalite in water or a mixture of water and water miscible solvent using alkali metal hydroxide and catalyst is disclosed herein. The present invention also discloses process for preparation of rabeprazole sulphide.

Abstract translation: 本发明公开了一种制备雷贝拉唑钠的方法，该方法包括使用碱金属氢氧化物和催化剂，在水或水和水混溶性溶剂的混合物中用次卤酸钠氧化湿的或干的雷贝拉唑硫化物。 本发明还公开了制备雷贝拉唑硫化物的方法。

公开(公告)号：WO2006024863A1

公开(公告)日：2006-03-09

申请号：PCT/GB2005/003392

申请日：2005-09-02

Applicant: CIPLA LIMITED ,  WAIN, Christopher, Paul ,  PATHI, Srinivas, Laxminarayan ,  PUPPALA, Ravikumar ,  KANKAN, Rajendra, Narayanrao ,  RAO, Dharmaraj, Ramchandra

Inventor： PATHI, Srinivas, Laxminarayan ,  PUPPALA, Ravikumar ,  KANKAN, Rajendra, Narayanrao ,  RAO, Dharmaraj, Ramchandra

IPC: C07D401/14 ,  A61K31/506 ,  A61P35/00

CPC classification number: C07D401/04

Abstract: The invention relates to a stable, non hygroscopic alpha crystalline form of methane sulfonic acid addition salt of 4-(4-methyl piperazin-lyl methyl)-N-[4-methyl-3-(4-pyridin-3-yl) pyrimidin-2-yl amino) phenyl]-benzamide (imatinib mesylate). A process for the preparation of the crystalline form is also described.

Abstract translation: 本发明涉及4-（4-甲基哌嗪 - 甲基）-N- [4-甲基-3-（4-吡啶-3-基）嘧啶的甲磺酸加成盐的稳定的非吸湿性α结晶形式 -2-基氨基）苯基] - 苯甲酰胺（甲磺酸伊马替尼）。 还描述了制备结晶形式的方法。

公开(公告)号：WO2012164242A8

公开(公告)日：2013-12-27

申请号：PCT/GB2012000480

申请日：2012-05-30

Applicant: CIPLA LTD ,  PUPPALA RAVIKUMAR ,  PATHI SRINIVAS LAXMINARAYAN ,  KANKAN RAJENDRA NARAYANRAO ,  COTTRILL EMILY ELIZABETH HELEN

Inventor： PUPPALA RAVIKUMAR ,  PATHI SRINIVAS LAXMINARAYAN ,  KANKAN RAJENDRA NARAYANRAO

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: The present invention provides a process for the preparation of paliperidone or a pharmaceutically acceptable salt thereof, wherein the process comprises condensing a compound of formula (II) with a compound of formula (III) or a salt thereof, in a suitable solvent and a base, in the presence of a catalyst and an inhibiting agent, wherein the inhibiting agent is added to the reaction system before the compound of formula (II) and compound of formula (III) have reacted or as the reaction of the compound of formula (II) and compound of formula (III) is initiated, and optionally converting the paliperidone to a salt thereof, wherein X is a suitable leaving group. The present invention also provides substantially pure paliperidone or a salt thereof, paliperidone or a salt thereof as prepared by the process and uses of the paliperidone or salt thereof.

Abstract translation: 本发明提供了一种制备普利培酮或其药学上可接受的盐的方法，其中所述方法包括在合适的溶剂和碱中将式（II）化合物与式（III）化合物或其盐缩合 在催化剂和抑制剂的存在下，其中在式（II）化合物和式（III）化合物已经反应之前或作为式（II）化合物的反应之前将该抑制剂加入到反应体系中 ）和式（III）的化合物引发，并且任选地将帕培酮转化成其盐，其中X是合适的离去基团。 本发明还提供了通过普利培酮或其盐的方法和用途制备的基本上纯的利培酮或其盐，普利培酮或其盐。