专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

21. 发明申请

WO2003101931A3 PREPARATION OF 4-(N, N-DISUBSTITUTEDAMINO) BUTYRALDEHYDE ACETALS 审中-公开
公开(公告)号：WO2003101931A3
公开(公告)日：2003-12-11
申请号：PCT/IN2003/000016
申请日：2003-02-03
申请人： NATCO PHARMA LIMITED , PULLA, Reddy, Muddasani , VENKAIAH, Chowdary, Nannapaneni
发明人： PULLA, Reddy, Muddasani , VENKAIAH, Chowdary, Nannapaneni
IPC分类号： C07C213/00
摘要： The invention disclosed in this application relates to an improved process for the preparation of compounds of formula (I): R 1 R 2 NCH 2 CH 2 CH 2 CH(OR 3 ) 2; wherein, R 1 = R 2 = C 1 -C 16 alkyl; C 3 -C 7 cycloalkyl; R 1 = C 1 -C 16 alkyl; R 2 = C 3 -C 7 cycloalkyl; NR 1 R 2 = pyrrolidino, piperidino, morpholino, thiomorpholino, R 1 = C 1 -C 6 alkyl; R 2 = ArCH 2 ; Ar =4-R 4 -C 6 H 4 -, R 4 = MeO, EtO, Me, Et, NMe 2 , NEt 2 , SMe, SEt, etc; R 3 =C 1 -C 6 alkyl; C 3 -C 7 cycloalkyl which comprises: (i) Reacting 3-(N, N-disubstitutedamino)propyl halide of formula (XXI): R 1 R 2 NCH 2 CH 2 CH 2 X; wherein, R 1 , R 2 = as defined above, X = C1 or Br, with magnesium in the presence of a solvent to get the Grrgnard reagent 3-(N, N-disubstitutedamino)-propylmagnesium halide; (ii) Reacting the resulting 3-(N, N-disubstitutedamino) propylmagnesium halide (Grignard reagent) with the trisubstituted orthoformate of formula (XVII): HC(OR 5 )(OR 3 ) 2 ; wherein, R 3 and R 5 is same or different and represent C 1 to C 6 alkyl, C 3 to C 7 cycloalkyl OR R 3 is as defined above and R 5 represents phenyl radical; (iii) Filtering off the resultant reaction mixture and distilling the filtrate to isolate the compound of the formula (I). These substituted butyraldehyde derivatives of the formula (I) are very important building blocks for the synthesis of various tryptamine derivatives. In particular 4-(N, N-dimethylamino)butyraldehyde dimethyl or diethyl acetals are crucial intermediates for the synthesis of commercially available anti-migraine drugs, like sumatriptan, zolmitriptan, and rizatriptan.

22. 发明申请

WO2009098715A2 NOVEL PYRAZOLO [3, 4 -D] PYRIMIDINE DERIVATIVES AS ANTI -CANCER AGENTS 审中-公开
标题翻译：新型吡唑并[3,4-d]嘧啶衍生物作为抗癌剂
公开(公告)号：WO2009098715A2
公开(公告)日：2009-08-13
申请号：PCT/IN2009/000037
申请日：2009-01-12
申请人： NATCO PHARMA LIMITED , KONAKANCHI, Durga, Prasad , PULA, Subba Rao , ANANTHANENI, Lakshmi , PILLI, Ramakrishna , PULLA REDDY, Muddasani , ADIBHATLA KALI SATYA, Bhujanga Rao , VENKAIAH CHOWDARY, Nannapaneni
发明人： KONAKANCHI, Durga, Prasad , PULA, Subba Rao , ANANTHANENI, Lakshmi , PILLI, Ramakrishna , PULLA REDDY, Muddasani , ADIBHATLA KALI SATYA, Bhujanga Rao , VENKAIAH CHOWDARY, Nannapaneni
CPC分类号： C07D487/04
摘要： The invention relates to substituted pyrazolo [3,4-d] pyrimidine derivatives of the Formula-(I), or pharmaceutically-acceptable salts thereof, which possess anti-proliferative activity such as anti-cancer activity and are accordingly useful in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of substituted pyrazolo [3,4-d] pyrimidine derivatives, to pharmaceutical compositions containing the compound and to its use in the manufacture of medicaments for the production of an anti- proliferative effect in a warm-blooded animal such as man.
摘要翻译：本发明涉及式（I）的取代的吡唑并[3,4-d]嘧啶衍生物或其药学上可接受的盐，其具有抗增殖活性，例如抗癌活性并因此可用于治疗人体或动物体的方法。本发明还涉及制备取代的吡唑并[3,4-d]嘧啶衍生物的方法，含有该化合物的药物组合物及其在制备用于在温血动物中产生抗增殖作用的药物中的用途，像人类这样的热血动物。

23. 发明申请

WO2008081477A1 3-ARYLOXY 3-SUBSTITUTED PROPANAMINES 审中-公开
标题翻译： 3-ARYLOXY 3-取代丙酰胺
公开(公告)号：WO2008081477A1
公开(公告)日：2008-07-10
申请号：PCT/IN2008/000001
申请日：2008-01-02
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , AJIT YASHWANT, Junnarkar , RAJASEKHARA, Reddy, Peddi , ADIBATLA KALI SATYA, Bhujanga, Rao , MADIREDDI, Umamaheshwar, Rao, Naidu , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , AJIT YASHWANT, Junnarkar , RAJASEKHARA, Reddy, Peddi , ADIBATLA KALI SATYA, Bhujanga, Rao , MADIREDDI, Umamaheshwar, Rao, Naidu , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07C217/72 , C07D211/22 , C07D295/092 , A61K31/205 , A61K31/452 , A61K31/5375 , A61P25/24
CPC分类号： C07D211/22 , C07C215/30 , C07C217/72 , C07C309/66 , C07D295/092
摘要： Present invention relates to novel 3-aryloxy 3-substituted propanamines of formula (I), method of preparing the same and to their use in inhibiting serotonin and norepinephrine reuptake wherein A is a phenyl which is optionally substituted with up to five substituents; a 1- or 2-naphthyl which is unsubstituted or substituted; a 5-membered heteroaryl radical which contains, as hetero atoms, 2 to 4 N-atoms or 1 or 2 N-atoms as well as 1 O- or S-atom, and which is unsubstituted or C-substituted by lower alkyl, phenyl, or substituted phenyl and/or is N-substituted at a N-atom which is capable of substitution by lower alkyl, lower alkoxy and/or halogen; a 2-benzimidazolyl optionally unsubstituted or substituted; and R 1 and R 2 are each independently hydrogen, C 1-6 -alkyl, C 3-7 -cycloalkyl, C 3-6 -cycloalkyl C 1-3 -alkyl; or R 1 and R 2 may together form a C 5-7 -carbocyclic ring containing 0-2 hetero atoms such as N, O, or S and a salt thereof with a pharmaceutically acceptable acid. Compounds of formula (I) (I-A: R=4-CF 3 , R 1 =H, R 2 =CH 3 , A=4-fluorophenyl), I-B: R=4-CF 3 , R 1 =H, R 2 =CH 3 , A=4-methylphenyl, I-C: R=4-CF 3 , R 1 =H, R 2 =CH3, A=4-methoxyphenyl) are found to be better than the antidepressant drug fluoxetine.
摘要翻译：本发明涉及式（I）的新型3-芳氧基3-取代丙胺，其制备方法及其在抑制5-羟色胺和去甲肾上腺素再摄取中的用途，其中A为任选被至多五个取代基取代的苯基; 未取代或取代的1-或2-萘基; 含有2至4个N原子或1或2个N原子以及1个O-或S-原子作为杂原子的5元杂芳基，其未被取代或被低级烷基取代，苯基或取代的苯基和/或在能够被低级烷基，低级烷氧基和/或卤素取代的N原子上被N-取代; 任选未取代或取代的2-苯并咪唑; 和R 1和R 2各自独立地为氢，C 1-6 - 烷基，C 3-7 环烷基，C 3-6 - 环烷基C 1-3 - 烷基; 或R 1和R 2可以一起形成含有0-2个杂原子的C 5〜5-碳环，例如N，O，或S及其盐与药学上可接受的酸。式（I）化合物（IA：R = 4-CF 3，R 1 = H，R 2 = CH 3 A = 4-氟苯基），IB：R = 4-CF 3，R 1 = H，R 2 = CH 3，A = 4-甲基苯基，IC：R = 4-CF 3，R 1 = H，R 2， / SUB> = CH3，A = 4-甲氧基苯基）比抗抑郁药物氟西汀更好。

24. 发明申请

WO2007039919A8 CRYSTALLINE FORMS OF ANASTROZOLE 审中-公开
标题翻译：晶体的晶体形式
公开(公告)号：WO2007039919A8
公开(公告)日：2007-12-06
申请号：PCT/IN2006000401
申请日：2006-10-06
申请人： NATCO PHARMA LTD , PULLA REDDY MUDDASANI , SAMBASIVA RAO TALASILA , VENKAIAH CHOWDARY NANNAPANENI
发明人： PULLA REDDY MUDDASANI , SAMBASIVA RAO TALASILA , VENKAIAH CHOWDARY NANNAPANENI
IPC分类号： C07D249/08 , A61K31/4196 , A61P35/00
CPC分类号： C07D249/08
摘要： The present invention relates to novel crystalline forms of anastrozole and processes for their preparation. Anastrozole is useful, as an anti-neoplastic agent in treatment of breast cancer. The novel forms have been designated by us as Forms I & Form II.
摘要翻译：本发明涉及阿那曲唑的新型结晶形式及其制备方法。阿那曲唑作为乳腺癌治疗中的抗肿瘤药物是有用的。这些小说形式已被我们指定为表格I和表格II。

25. 发明申请

WO2007013097A8 IMPROVED PROCESS FOR THE PREPARATION OF IBANDRONATE SODIUM 审中-公开
标题翻译：改进IBANDRONATE SODIUM的制备方法
公开(公告)号：WO2007013097A8
公开(公告)日：2007-12-06
申请号：PCT/IN2006000251
申请日：2006-07-17
申请人： NATCO PHARMA LTD , PULLA REDDY MUDDASANI , USHARANI VATTIKUTI , VENKAIAH CHOWDARY NANNAPANENI
发明人： PULLA REDDY MUDDASANI , USHARANI VATTIKUTI , VENKAIAH CHOWDARY NANNAPANENI
IPC分类号： C07F9/38
CPC分类号： C07F9/3873
摘要： Present invention discloses an improved and commercial process for the preparation of ibandronic acid or its monosodium salt. According to the process 3-N-methylaminopropionitrile is reacted with n-pentylbromide to get the tertiary amine of formula-II. Hydrolysis of the nitrile compound of formula-II with hydrochloric acid gave the b-alanine derivative of formula-X. Bis-phosphonylation of the acid compound of formula-X with phorphorous trichloride and phosphorous acid, followed by water hydrolysis gave aqueous ibandronic acid. Treatment of this with sodium hydroxide, followed by dilution of the aqueous solution with methanol gave ibandronate monosodium of formula-Ia as white crystalline solid. Present process utilizes simple raw materials and avoids the column chromatography technique used in the prior art process for isolation of ibandronic acid. Overall yield of ibandronate is more than 60% from the nitrile intermediate of formula-II. Ibandronate is widely used as bone resorption inhibitor.
摘要翻译：本发明公开了用于制备伊班膦酸或其单钠盐的改进和商业化方法。根据方法，将3-N-甲基氨基丙腈与正戊基溴反应得到式II的叔胺。用盐酸水解式II的腈化合物得到式-X的β-丙氨酸衍生物。将式-X的酸化合物与无色三氯化磷和亚磷酸二膦酰化，随后进行水解，得到伊班膦酸水溶液。用氢氧化钠处理，然后用甲醇稀释水溶液，得到式Ia的伊班膦酸钠单钠为白色结晶固体。本发明方法使用简单的原料，并避免了用于分离伊班膦酸的现有技术方法中使用的柱色谱技术。伊班膦酸钠的总收率高于式Ⅱ的腈中间体的60％以上。伊班膦酸盐被广泛用作骨吸收抑制剂。

26. 发明申请

WO2007074475A2 NOVEL POLYMORPHIC FORMS OF IBANDRONATE 审中-公开
标题翻译：新型IBANDRONATE多晶型
公开(公告)号：WO2007074475A2
公开(公告)日：2007-07-05
申请号：PCT/IN2006/000501
申请日：2006-12-21
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , USHARANI, Vattikuti , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , USHARANI, Vattikuti , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07F9/38 , A61K31/663
CPC分类号： C07F9/3873
摘要： The present invention relates to novel and stable polymorphic forms of ibandronate monosodium monohydrate of formula I and processes for their preparation. Ibandronate monosodium monohydrate is useful, as bone resorption inhibitor. The novel crystalline forms are designated as Form I, Form II and the amorphous ibandronate monosodium monohydrate as Form III.
摘要翻译：本发明涉及式I的伊班膦酸一钠一水合物的新颖且稳定的多晶型形式及其制备方法。伊班膦酸单钠一水合物作为骨吸收抑制剂是有用的。新的结晶形式被指定为形式I，形式II和无定形伊班膦酸钠一水合物形式III。

27. 发明申请

WO2007039919A1 CRYSTALLINE FORMS OF ANASTROZOLE 审中-公开
标题翻译： ANASTROZOLE的结晶形式
公开(公告)号：WO2007039919A1
公开(公告)日：2007-04-12
申请号：PCT/IN2006/000401
申请日：2006-10-06
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , SAMBASIVA RAO, Talasila , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , SAMBASIVA RAO, Talasila , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D249/08 , A61K31/4196 , A61P35/00
CPC分类号： C07D249/08
摘要： The present invention relates to novel crystalline forms of anastrozole and processes for their preparation. Anastrozole is useful, as an anti-neoplastic agent in treatment of breast cancer. The novel forms have been designated by us as Forms I & Form II.
摘要翻译：本发明涉及阿那曲唑的新型结晶形式及其制备方法。阿那曲唑作为治疗乳腺癌的抗肿瘤药物是有用的。这些新颖的形式已被我们指定为表格I＆amp; 表格II。

28. 发明申请

WO2006025071A1 A PROCESS FOR THE PREPARATION OF ESCITALOPRAM 审中-公开
标题翻译：编制ESCITALOPRAM的过程
公开(公告)号：WO2006025071A1
公开(公告)日：2006-03-09
申请号：PCT/IN2005/000282
申请日：2005-08-23
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , SAMBASIVA RAO, Talasila , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , SAMBASIVA RAO, Talasila , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D307/87
CPC分类号： C07D307/87
摘要： The present invention relates to an improved process for the preparation of escitalopram of the formula-(I) which consists of a sequential double Grignard reaction on 5-iodophthalide to get the dihydroxy compound of formula-(XVI), its resolution using a chiral acid, cyclization of resolved compound of the formula-(XVII), and cyanation of compound of the formula-(XVIII) using DMF and copper (I) cyanide. The present process utilizes the facile displacement of iodo group with cyano group in the final step of escitalopram. Escitalopram is a widely used anti-depressant.
摘要翻译：本发明涉及一种制备式（I）的依他普仑的改进方法，其由在5-碘苯酞上的顺序双格氏反应组成，得到式 - （XVI）的二羟基化合物，其使用手性酸的分辨率，使用DMF和氰化铜（I）使式 - （XVII）的分解化合物环化并得到式 - （XVIII）化合物的氰化。本方法利用在依他普仑最终步骤中碘基与氰基的轻易置换。艾司西酞普兰是广泛使用的抗抑郁药。

29. 发明申请

WO2005105762A1 IMPROVED PROCESS FOR THE PREPARATION OF HIGH PURITY ANASTROZOLE 审中-公开
标题翻译：用于制备高纯度阿诺唑的改进方法
公开(公告)号：WO2005105762A1
公开(公告)日：2005-11-10
申请号：PCT/IN2005/000140
申请日：2005-05-04
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D249/08
CPC分类号： C07D249/08
摘要： Present invention discloses an improved process for the preparation of high purity anastrozole of formula-I (2,2'-[5-(1H-1,2,4-triazol-1-ylmethyl)-1,3-phenylene]di(2-methylpropio-nitrile) consisting of: (i) halogenation of 5, α, α, α', α'-pentamethyl-1,3-benzenediacetonitrile; (ii) reaction with sodium/potassium triazole; (iii) purification of crude anastrozole (containing more than 1% of triazole isomeric impurity) through salt formation; and (iv) isolation of pure anastrozole from its salts. It is observed that the removal of triazole isomeric impurity is possible only through a salt formation.
摘要翻译：本发明公开了一种改进的制备式I（2,2' - [5-（1H-1,2,4-三唑-1-基甲基）-1,3-亚苯基]二（由（ⅰ）5，α，α，α'，α'-五甲基-1,3-苯二乙腈卤化;（ⅱ）与钠/钾三唑反应;（ⅲ）纯化粗品阿那曲唑（含有超过1％的三唑异构杂质）通过盐形成;和（iv）从其盐分离纯阿那曲唑。观察到三唑异构杂质的去除仅可通过盐形成。

30. 发明申请

WO2005070909A1 AN IMPROVED PROCESS FOR THE PREPARATION OF GEFITINIB 审中-公开
标题翻译：改进GEFITINIB的制备方法
公开(公告)号：WO2005070909A1
公开(公告)日：2005-08-04
申请号：PCT/IN2004/000223
申请日：2004-07-27
申请人： NATCO PHARMA LIMITED , JYOTHI PRASAD, Ramanadham , PULLA REDDY, Muddasani , NAGESHWARA RAO, Bollepalli , VENKAIAH CHOWDARY, Nannapaneni
发明人： JYOTHI PRASAD, Ramanadham , PULLA REDDY, Muddasani , NAGESHWARA RAO, Bollepalli , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07D295/08
CPC分类号： C07D295/088 , C07D239/94
摘要： Present invention discloses an improved process for the preparation of gefitinib (4-(3'-chloro-4'-fluorophenylamino)-7-methoxy-6-[3-(4-morpholinyl)propoxy]quinazoline), of formula-I, which comprises: (i) etherification of iso-vanillin with 3-morpholinopropyl halide, (ii) nitration using nitric acid, (iii) oximation, (iv) dehydration, (v) reduction-cum-hydrolysis, (vi) quinazolinone formation, (vii) introduction of a leaving group at C-4 position in quinozolinone, and (viii) condensation with 3-chloro4-fluoroaniline to get the crude gefitinib. Purification of crude gefitinib is achieved via acid/base treatment or by crystallization from solvents such as ethyl acetate, isopropanol, acetonitrile, and methyl ethyl ketone. Formula I, IX, XI, XIII, XV and XVI.
摘要翻译：本发明公开了制备式I的吉非替尼（4-（3'-氯-4'-氟苯基氨基）-7-甲氧基-6- [3-（4-吗啉基）丙氧基]喹唑啉）的改进方法，其包括：（i）异香兰素与3-吗啉代丙基卤化物的醚化，（ii）使用硝酸的硝化，（iii）肟化，（iv）脱水，（v）还原 - 并 - 水解，（vi）喹唑啉酮形成，（vii）在喹诺酮中的C-4位置引入离去基团，和（viii）与3-氯-4-氟苯胺缩合得到粗制吉非替尼。粗制吉非替尼的纯化通过酸/碱处理或通过从溶剂如乙酸乙酯，异丙醇，乙腈和甲基乙基酮中结晶来实现。式I，IX，XI，XIII，XV和XVI。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式