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21. 发明授权

US09895367B2 Formulation comprising phenylaminopyrimidine derivative as active agent 有权
公开(公告)号：US09895367B2
公开(公告)日：2018-02-20
申请号：US14003445
申请日：2011-08-10
申请人： Durga Maheswari Parvataneni , Siddhartha Yedluri , Venkata Satyanarayana Appadwedula , Kali Satya Bhujanga Rao , Venkaiah Chowdary Nannapaneni
发明人： Durga Maheswari Parvataneni , Siddhartha Yedluri , Venkata Satyanarayana Appadwedula , Kali Satya Bhujanga Rao , Venkaiah Chowdary Nannapaneni
IPC分类号： A61K31/506 , A61K9/107 , A61K9/00 , A61K9/48 , A61K47/10 , A61K47/14 , A61K9/08 , A61K47/44
CPC分类号： A61K31/506 , A61K9/0053 , A61K9/08 , A61K9/107 , A61K9/4858 , A61K9/4866 , A61K47/10 , A61K47/14 , A61K47/44
摘要： An oral pharmaceutical formulation containing an effective amount of NRC-AN-019 including its pharmaceutically acceptable salts and polymorphs such as Form I, Form II and Form III thereof to improve the bioavailability intended for self-emulsification upon its contact with the gastro-intestinal fluid. The invention also relates to a process for the preparation of oral solution containing NRC-AN-019 in an effective concentration for the better therapy against Chronic Myeloid Leukemia as BCR-ABL tyrosine kinase inhibitor and against other tumors such as head and neck cancer, prostate cancer and the like.

22. 发明授权

US09440959B2 Process for the preparation of nilotinib 有权
标题翻译：尼罗替尼的制备方法
公开(公告)号：US09440959B2
公开(公告)日：2016-09-13
申请号：US14660628
申请日：2015-03-17
申请人： Natco Pharma Limited
发明人： Amala Kompella , Adibhatla Kali Satya Bhujanga Rao , Sreenivas Rachakonda , Venugopala Krishna Gampa , Venkaiah Chowdary Nannapaneni
IPC分类号： C07D401/14 , A61K31/506 , C07D233/61
CPC分类号： C07D401/14 , A61K31/506 , C07B2200/13 , C07D233/61
摘要： The present invention relates a process for the preparation of a compound of formula (I): or a pharmaceutically acceptable salt thereof, which process comprises converting a compound of formula (IV): or a pharmaceutically acceptable salt thereof, into the compound of formula (I) or a pharmaceutically acceptable salt thereof.

23. 发明授权

US09227948B2 Process for the preparation of 2-substituted-2-(6-(substituted)-7-methylbenzo[D][1,3]dioxol-4-yl)acetic acid derivatives 有权
标题翻译：制备2-取代-2-（6-（取代的）-7-甲基苯并[D] [1,3]间二氧杂环戊烯-4-基）乙酸衍生物的方法
公开(公告)号：US09227948B2
公开(公告)日：2016-01-05
申请号：US14408534
申请日：2013-06-19
申请人： Natco Pharma Limited
发明人： Pulla Reddy Muddasani , Manikumar Chintalapudi , Venkaiah Chowdary Nannapaneni
IPC分类号： C07D309/12 , C07D317/64 , C07F7/18 , C07C43/23 , C07C59/64 , C07C69/734
CPC分类号： C07D317/64 , C07C43/23 , C07C59/64 , C07C69/734 , C07D309/12 , C07F7/1804 , Y02P20/55
摘要： Present invention relates to an improved and commercial process for the preparation of 2-sustituted-2-(6-(substituted)-7-methylbenzo[d][1,3]dioxol-4-yl)acetic acid derivatives of formula-I the above Formula I, XII, XIII, XV, wherein R1 is a O-protecting group such as methoxymethyl, ethoxymethyl, trialkylsilyl, arylmethyl, tetrahydropyran-2-yl, allyl; X is hydroxyl, halogen, mesylate, triflate, tosylate, acetate; Y is oxygen atom, NH or sulfur atom; R2 is C1-C6 alkyl. 2,4-Dihydroxy-3-methylbenzaldehyde is selectively protected at C-4 position in the form of an ether compound of formula-XII, oxidized the aldehyde function to get the diol of formula-XIII, and condensed with ethyl glyoxalate under Casiraghi reaction conditions to get the compound of formula-XV. Compound of formula-XV is converted to compound of formula-I by conventional chemistry. Compounds of formula-I are key intermediates in the synthesis of ecteinascidines like trabectedin.
摘要翻译：本发明涉及制备式I的2-取代-2-（6-（取代的）-7-甲基苯并[d] [1,3]二氧杂环戊烯-4-基）乙酸衍生物的改进和商业化方法上述式I，XII，XIII，XV，其中R 1是O-保护基如甲氧基甲基，乙氧基甲基，三烷基甲硅烷基，芳基甲基，四氢吡喃-2-基，烯丙基; X是羟基，卤素，甲磺酸酯，三氟甲磺酸酯，甲苯磺酸酯，乙酸酯; Y是氧原子，NH或硫原子; R2是C1-C6烷基。 2,4-二羟基-3-甲基苯甲醛在C-4位被选择性保护为式-IIII的醚化合物形式，氧化醛官能团以得到式-IIIIII的二醇，并在卡西拉希反应下与乙二醛酸乙酯缩合得到式XV化合物的条件。通过常规化学方法将式XV的化合物转化为式I的化合物。式I的化合物是合成类似于trabectinin的ecteinascidine的关键中间体。

24. 发明授权

US08501962B2 Process for the preparation of high purity sunitinib and its pharmaceutically acceptable salt 失效
标题翻译：制备高纯度舒尼替尼及其药学上可接受的盐的方法
公开(公告)号：US08501962B2
公开(公告)日：2013-08-06
申请号：US13000126
申请日：2008-11-17
申请人： Srinivasa Krishna Murthy Konduri , Bhujanga Rao Adibhatla Kali Satya , Nannapaneni Venkaiah Chowdary
发明人： Srinivasa Krishna Murthy Konduri , Bhujanga Rao Adibhatla Kali Satya , Nannapaneni Venkaiah Chowdary
IPC分类号： C07D209/34
CPC分类号： C07D403/06 , Y02P20/582
摘要： The present invention relates to an improved process for the preparation of N-[2-(diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidine)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide—Sunitinib base of formula (I) and its pharmaceutically acceptable malate salt of formula (I(a)).
摘要翻译：本发明涉及制备N- [2-（二乙基氨基）乙基] -5 - [（Z） - （5-氟-1,2-二氢-2-氧代-3H-吲哚-3 - 哌啶）甲基] -2,4-二甲基-1H-吡咯-3-甲酰胺 - 式（I）的舒尼替尼碱及其药学上可接受的式（I（a））的苹果酸盐。

25. 发明申请

US20130060030A1 PROCESS FOR THE PREPARATION OF HIGHLY PURE CRYSTALLINE IMATINIB BASE 审中-公开
标题翻译：制备高纯度晶体基质的方法
公开(公告)号：US20130060030A1
公开(公告)日：2013-03-07
申请号：US13634725
申请日：2010-03-15
申请人： Amalia Kompella , Kali Satya Bhujanga Rao Adibhatla , Sreenivas Rachakonda , Venkaiah Chowdary Nannapeneni
发明人： Amalia Kompella , Kali Satya Bhujanga Rao Adibhatla , Sreenivas Rachakonda , Venkaiah Chowdary Nannapeneni
IPC分类号： C07D403/14
CPC分类号： C07D401/04
摘要： A process for the preparation of highly pure crystalline imatinib base form- N of Formula (I) is disclosed. Imatinib base of this invention is suitable for conversion to pharmaceutically acceptable salts.
摘要翻译：公开了制备式（I）的高纯度结晶伊马替尼碱形式-N的方法。本发明的伊马替尼碱适于转化成药学上可接受的盐。

26. 发明申请

US20120172380A1 NOVEL 4-(TETRAZOL-5-YL)-QUINAZOLINE DERIVATIVES AS ANTI CANCER AGENT 审中-公开
标题翻译：新4-（TETRAZOL-5-YL） - 喹诺酮衍生物作为抗癌剂
公开(公告)号：US20120172380A1
公开(公告)日：2012-07-05
申请号：US13330304
申请日：2011-12-19
申请人： Durga prasad Konakanchi , Subba Rao Pula , Lakshmi Ananthaneni , Pulla Reddy Muddasani , Kali Satya Bhujanga Rao Adibhatla , Venkaiah Chowdary Nannapaneni
发明人： Durga prasad Konakanchi , Subba Rao Pula , Lakshmi Ananthaneni , Pulla Reddy Muddasani , Kali Satya Bhujanga Rao Adibhatla , Venkaiah Chowdary Nannapaneni
IPC分类号： A61K31/517 , A61P35/00
CPC分类号： A61K31/517
摘要： The invention relates to substituted 4-(tetrazol-5-yl)-quinazoline 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 4-(tetrazol-5-yl)-quinazoline 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：本发明涉及具有抗增殖活性如抗癌活性的式I的取代的4-（四唑-5-基） - 喹唑啉衍生物或其药学上可接受的盐，因此可用于治疗人或动物的身体。本发明还涉及制备取代的4-（四唑-5-基） - 喹唑啉衍生物的方法，用于制备含有该化合物的药物组合物及其在制备药物中的用途，所述药物在其中产生抗增殖作用温血动物如人。

27. 发明授权

US08080558B2 4-(tetrazol-5-yl)-quinazoline derivatives as anti-cancer agent 失效
标题翻译： 4-（四唑-5-基） - 喹唑啉衍生物作为抗癌剂
公开(公告)号：US08080558B2
公开(公告)日：2011-12-20
申请号：US12740527
申请日：2008-10-28
申请人： Durga Prasad Konakanchi , Subba Rao Pula , Lakshmi Ananthaneni , Muddasani Pulla Reddy , Bhujanga Rao Adibhatla Kali Satya , Nannapaneni Venkaiah Chowdary
发明人： Durga Prasad Konakanchi , Subba Rao Pula , Lakshmi Ananthaneni , Muddasani Pulla Reddy , Bhujanga Rao Adibhatla Kali Satya , Nannapaneni Venkaiah Chowdary
IPC分类号： A61K31/517
CPC分类号： C07D403/04 , C07D239/72 , C07D239/86 , C07D239/94 , C07D401/14 , C07D403/14
摘要： The invention relates to substituted 4-(tetrazol-5-yl)-quinazoline 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 4-(tetrazol-5-yl)-quinazoline 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：本发明涉及具有抗增殖活性如抗癌活性的式I的取代的4-（四唑-5-基） - 喹唑啉衍生物或其药学上可接受的盐，因此可用于治疗方法的人体或动物体。本发明还涉及制备取代的4-（四唑-5-基） - 喹唑啉衍生物的方法，用于制备含有该化合物的药物组合物及其在制备药物中的用途，所述药物在其中产生抗增殖作用温血动物如人。

28. 发明授权

US08048883B2 Polymorphic form of imatinib mesylate and a process for its preparation 有权
标题翻译：伊马替尼甲磺酸多形态及其制备方法
公开(公告)号：US08048883B2
公开(公告)日：2011-11-01
申请号：US10585702
申请日：2004-11-16
申请人： Kompella Amala , Thungathurthi Srinivasa Rao , Bhujanga rao Adibhatla Kali Satya , Sreenivas Rachakonda , Nannapaneni Venkaiah Chowdary , Khadgapathi Podili
发明人： Kompella Amala , Thungathurthi Srinivasa Rao , Bhujanga rao Adibhatla Kali Satya , Sreenivas Rachakonda , Nannapaneni Venkaiah Chowdary , Khadgapathi Podili
IPC分类号： A01N43/58 , A61K31/50 , C07D239/02
CPC分类号： C07D401/04
摘要： This invention discloses a novel stable crystal form of imatinib mesylate, designated by us as α2 Form, which is stable at room temperature and even at higher temperatures up to 120° C. and accelerated stress conditions and, freely soluble in water. This invention also discloses a pharmaceutical composition containing the novel stable α2 form of Imatinib mesylate and other usually employed excipients, useful in the treatment of Chronic Myelogenous Leukemia (CML). This new α2 Form of imatinib mesylate is prepared by slurrying Imatinib base in isopropanol at room temperature followed by addition of methane sulfonic acid and maintaining 50-60 ° C. followed by filtration. This invention also discloses another process for the preparation of the novel, stable α2 crystalline form of Imatinib Mesylate by the conversion of Imatinib mesylate β-polymorphic modification by suspending it in water and organic solvents, distilling off water azeotropically, cooling and filtering to obtain the α2 crystal form.
摘要翻译：本发明公开了一种新颖的甲磺酸伊马替尼结晶形式，由我们称为α2形式，其在室温下甚至在高达120℃的较高温度下是稳定的，并且加速应激条件并且易溶于水。本发明还公开了一种药物组合物，其含有可用于治疗慢性骨髓性白血病（CML）的新型稳定α2形式的甲磺酸伊马替尼和其它通常使用的赋形剂。这种新的α2甲磺酸伊马替尼形式是通过在室温下将伊马替尼碱分散在异丙醇中制备的，然后加入甲磺酸并保持50-60℃，然后过滤。本发明还公开了通过将甲磺酸伊马替尼和bgr-多晶型修饰物悬浮在水和有机溶剂中，通过共沸蒸馏除去水，冷却和过滤来制备新型稳定的α2结晶形式的伊马替尼甲磺酸盐的另一种方法，以获得 α2晶体形式。

29. 发明申请

US20110263852A1 NOVEL PROCESS FOR THE PREPARATION OF LAPATINIB AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS 失效
标题翻译：制备LAPATINIB及其药物接受口服的新方法
公开(公告)号：US20110263852A1
公开(公告)日：2011-10-27
申请号：US13127042
申请日：2009-08-12
申请人： Ramanadham Jyothi Prasad , Bhujanga Rao Adibhatla Kali Satya , Nannapaneni Venkaiah Chowdary
发明人： Ramanadham Jyothi Prasad , Bhujanga Rao Adibhatla Kali Satya , Nannapaneni Venkaiah Chowdary
IPC分类号： C07D407/10 , C07C251/00
CPC分类号： C07D239/94 , C07C257/12 , C07D405/04
摘要： The present invention relates to an improved and novel process for the preparation of high purity crystalline base of Lapatinib of formula-(1) having chemical name N-{3-chloro-4-[(3-fluorobenzyloxy]phenyl}-6-[5-({[2-(methanesulfonyl)ethyl]amino}methyl]-2-furyl]-4-quin-azolinamine and its pharmaceutically acceptable salts. The present invention further relates to intermediates according to formula (8) and formula (9) used in this process
摘要翻译：本发明涉及一种制备具有化学名称为N- {3-氯-4 - [（3-氟苄氧基）苯基} -6- [ 5 - （{[2-（甲磺酰基）乙基]氨基}甲基] -2-呋喃基] -4-喹唑啉胺及其药学上可接受的盐本发明还涉及根据式（8）和式）

30. 发明申请

US20110028473A1 METHODS OF TREATING DRUG RESISTANT AND OTHER TUMORS BY ADMINISTERING 6,7-DIALKOXY QUINAZOLINE DERIVATIVES 有权
标题翻译：通过管理6,7-二烷氧基喹唑啉衍生物治疗耐药菌及其他肿瘤的方法
公开(公告)号：US20110028473A1
公开(公告)日：2011-02-03
申请号：US12833733
申请日：2010-07-09
申请人： Bhujanga rao ADIBHATLA KALI SATYA , Ramanadham JYOTHI PRASAD , Bollepalli NAGESHWARA RAO , Nannapaneni VENKAIAH CHOWDARY
发明人： Bhujanga rao ADIBHATLA KALI SATYA , Ramanadham JYOTHI PRASAD , Bollepalli NAGESHWARA RAO , Nannapaneni VENKAIAH CHOWDARY
IPC分类号： A61K31/517 , A61K31/5377 , A61P35/00
CPC分类号： A61K31/517
摘要： Methods employing and uses of a compound of formula (I) in inhibiting the growth of a tumor cell in a subject in need thereof. Methods employing and uses of a compound of formula (I) in treating pancreatic cancer in a subject in need of treatment for pancreatic cancer. Methods employing and uses of a compound of formula (I) in treating HER-2 positive breast cancer in a subject in need of treatment for HER-2 positive breast cancer. Methods employing and uses of a compound of formula (I) in treating drug resistant non-small cell lung cancer in a subject in need of treatment for drug resistant non-small cell lung cancer. Each of these methods can include administering to the subject an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.Method of manufacturing a medicament including a compound of formula (I) for treating a subject suffering from growth of a tumor cell; for treating a subject suffering from pancreatic cancer; for treating a subject suffering from HER-2 positive breast cancer; or for treating a subject suffering from drug resistant non-small cell lung cancer.
摘要翻译：使用和使用式（I）化合物抑制有需要的受试者中肿瘤细胞生长的方法。在需要治疗胰腺癌的受试者中使用和使用式（I）化合物治疗胰腺癌的方法。在需要治疗HER-2阳性乳腺癌的受试者中使用和使用式（I）化合物治疗HER-2阳性乳腺癌的方法。在需要治疗耐药性非小细胞肺癌的受试者中使用和使用式（I）化合物在治疗耐药性非小细胞肺癌中的方法。这些方法中的每一种可以包括向受试者施用有效量的式（I）化合物或其药学上可接受的盐。制备药物的方法，所述药物包括用于治疗患有肿瘤细胞生长的受试者的式（I）化合物; 用于治疗患有胰腺癌的受试者; 用于治疗患有HER-2阳性乳腺癌的受试者; 或用于治疗患有耐药非小细胞肺癌的受试者。

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