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1. 发明授权

US07960545B2 Process for the prepartion of erlotinib 有权
标题翻译：厄洛替尼的制备过程
公开(公告)号：US07960545B2
公开(公告)日：2011-06-14
申请号：US12094926
申请日：2006-11-22
申请人： Ramanadham Jyothi Prasad , Bollepalli Nageshwar Rao , Nannapaneni Venkaiah Chowdary
发明人： Ramanadham Jyothi Prasad , Bollepalli Nageshwar Rao , Nannapaneni Venkaiah Chowdary
IPC分类号： C07D239/72
CPC分类号： C07D239/94
摘要： The present invention discloses an improved and novel process for the preparation of erlotinib (N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine) of formula (1), which comprises: (i) demethylation of commercially available 6,7-dimethoxy-4(3H)-quinazolinone of formula (8); acetylation using acetic anhydride; (iii) introduction of a leaving group at C-4 position in quinazolinone; (iv) condensation with 3-ethynylaniline to get novel compound of formula (12); (v) deacetylation to get novel dihydroxy compound of formula (13); and (vi) O-alkylation with 2-iodoethylmethyl ether to get the erlotinib base of formula (1). Erlotinib base is purified by recrystallization from ethyl acetate to get a HPLC purity of >99.5%. Salt formation of this base with hydrogen chloride gave pharmaceutically acceptable erlotinib hydrochloride of formula (1a) with a HPLC purity of >99.8%. Erlotinib hydrochloride is useful for the treatment of proliferative disorders, such as cancers, in humans.
摘要翻译：本发明公开了一种制备式（1）的厄洛替尼（N-（3-乙炔基苯基）-6,7-双（2-甲氧基乙氧基）-4-喹唑啉胺）的改进和新颖的方法，其包括：（i）市售的式（8）的6,7-二甲氧基-4（3H） - 喹唑啉酮的脱甲基化; 使用乙酸酐乙酰化; （iii）在喹唑啉酮的C-4位引入离去基团; （iv）与3-乙炔基苯胺缩合得到新的式（12）化合物; （v）脱乙酰化得到式（13）的新型二羟基化合物; 和（vi）用2-碘乙基甲基醚O-烷基化得到式（1）的厄洛替尼碱。埃洛替尼碱通过乙酸乙酯重结晶纯化，得到HPLC纯度> 99.5％。用氯化氢盐形成该碱，得到HPLC纯度> 99.8％的药学上可接受的式（1a）盐酸阿洛替尼。盐酸埃罗替尼可用于治疗人类增殖性疾病，如癌症。

2. 发明申请

US20110039844A1 6-7,DIALKOXY QUINAZOLINE DERIVATIVES USEFUL FOR TREATMENT OF CANCER RELATED DISORDERS 有权
标题翻译： 6-7，适用于治疗癌症相关疾病的DIALKOXY喹唑啉衍生物
公开(公告)号：US20110039844A1
公开(公告)日：2011-02-17
申请号：US12812726
申请日：2008-01-18
申请人： Ramanadham Jyothi Prasad , Bhujanga Rao Adibhatla Satya , Bollepalli Nageshwar Rao , Nannapaneni Venkaiah Chowdary
发明人： Ramanadham Jyothi Prasad , Bhujanga Rao Adibhatla Satya , Bollepalli Nageshwar Rao , Nannapaneni Venkaiah Chowdary
IPC分类号： A61K31/5377 , C07D413/12 , A61P35/00
CPC分类号： A61K31/5377 , C07D239/94
摘要： In view of the great potential the quinazoline class of compounds offer, we started the synthesis and screening of a large number of new chemical entities with novel structural features. It has been surprisingly and unexpectedly found that quinazolines having 3-Ethynyl anilino group at the 4th position and specifically substituted alkoxy groups in the 6 and 7 positions, impart much enhanced and special anti-proliferative properties when compared to other prominent members of the quinazoline class of drugs. Also, surprisingly the compounds of this invention are much less toxic and the safety profile is exceedingly beneficial for therapeutic applications. The novel chemical entities described in this invention are designated by the general structure (I) and have not been synthesized earlier nor investigated for their therapeutic benefits and safety profile. Compound (I) is NRC-2694, when structure (A).
摘要翻译：鉴于喹唑啉类化合物具有巨大的潜力，我们开始对大量具有新型结构特征的新化学物质进行合成和筛选。出人意料地发现，与喹唑啉类的其他显着成分相比，在第4位具有3-乙炔基苯胺基的6和7位上具有特异性取代的烷氧基的喹唑啉具有很强的增强和特殊的抗增殖特性的药物。此外，令人惊讶的是，本发明的化合物毒性远低于安全性，对于治疗应用是非常有益的。本发明中描述的新颖化学实体由通式结构（I）表示，并没有早期合成，也没有对其治疗益处和安全性进行调查。当结构（A）时，化合物（I）是NRC-2694。

3. 发明申请

US20090306377A1 NOVEL PROCESS FOR THE PREPARTION OF ERLOTINIB 有权
标题翻译：用于制备ERLOTINIB的新方法
公开(公告)号：US20090306377A1
公开(公告)日：2009-12-10
申请号：US12094926
申请日：2006-11-22
申请人： Ramanadham Jyothi Prasad , Bollepalli Nageshwar Rao , Nannapaneni Venkaiah Chowdary
发明人： Ramanadham Jyothi Prasad , Bollepalli Nageshwar Rao , Nannapaneni Venkaiah Chowdary
IPC分类号： C07D239/94
CPC分类号： C07D239/94
摘要： The present invention discloses an improved and novel process for the preparation of erlotinib (N-(3-ethynylphenyl)-6,7-bis(2-methoxyethoxy)-4-quinazolinamine) of formula (1), which comprises: (i) demethylation of commercially available 6,7-dimethoxy-4(3H)-quinazolinone of formula (8); acetylation using acetic anhydride; (iii) introduction of a leaving group at C-4 position in quinazolinone; (iv) condensation with 3-ethynylaniline to get novel compound of formula (12); (v) deacetylation to get novel dihydroxy compound of formula (13); and (vi) O-alkylation with 2-iodoethylmethyl ether to get the erlotinib base of formula (1). Erlotinib base is purified by recrystallization from ethyl acetate to get a HPLC purity of >99.5%. Salt formation of this base with hydrogen chloride gave pharmaceutically acceptable erlotinib hydrochloride of formula (1a) with a HPLC purity of >99.8%. Erlotinib hydrochloride is useful for the treatment of proliferative disorders, such as cancers, in humans.
摘要翻译：本发明公开了一种制备式（1）的厄洛替尼（N-（3-乙炔基苯基）-6,7-双（2-甲氧基乙氧基）-4-喹唑啉胺）的改进和新颖的方法，其包括：（i）市售的式（8）的6,7-二甲氧基-4（3H） - 喹唑啉酮的脱甲基化; 使用乙酸酐乙酰化; （iii）在喹唑啉酮的C-4位引入离去基团; （iv）与3-乙炔基苯胺缩合得到新的式（12）化合物; （v）脱乙酰化得到式（13）的新二羟基化合物; 和（vi）用2-碘乙基甲基醚O-烷基化得到式（1）的厄洛替尼碱。埃洛替尼碱通过乙酸乙酯重结晶纯化，得到HPLC纯度> 99.5％。用氯化氢盐形成该碱，得到HPLC纯度> 99.8％的药学上可接受的式（1a）盐酸阿洛替尼。盐酸埃罗替尼可用于治疗人类增殖性疾病，如癌症。

4. 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）

5. 发明授权

US08349855B2 Polymorphs of erlotinib hydrochloride and method of preparation 有权
标题翻译：盐酸厄洛替尼的多晶型物及其制备方法
公开(公告)号：US08349855B2
公开(公告)日：2013-01-08
申请号：US12672191
申请日：2007-09-11
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： A61K31/517
CPC分类号： C07D239/94
摘要： The present invention relates to three novel crystalline forms of Erlotinib hydrochloride and method of preparation thereof. Erlotinib hydrochloride is N-(3-ethynylphenyl)-6,7-bis(2-methoxy ethoxy)-4-quinazolinamine hydrochloride of formula-(I). The present invention provides stable novel crystalline forms of Erlotinib hydrochloride designated as Form-M, Form-N and Form-P, and processes for the preparation of the same. Erlotinib hydrochloride can be used as medicament for the treatment of hyperproliferative disorders, such as cancers, in humans.
摘要翻译：本发明涉及盐酸埃洛替尼的三种新型结晶形式及其制备方法。盐酸埃洛替尼是式（I）的N-（3-乙炔基苯基）-6,7-双（2-甲氧基乙氧基）-4-喹唑啉胺盐酸盐。本发明提供了称为Form-M，Form-N和Form-P的盐酸埃罗替尼的稳定新型结晶形式及其制备方法。盐酸埃洛替尼可用作治疗人类过度增生性疾病如癌症的药物。

6. 发明授权

US08664389B2 Process for the preparation of lapatinib and it's pharmaceutically acceptable salts 失效
标题翻译：制备拉帕替尼及其药学上可接受的盐的新方法
公开(公告)号：US08664389B2
公开(公告)日：2014-03-04
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： C07C257/12 , C07C251/00 , C07D239/94 , C07D405/04 , C07D407/10
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）。

7. 发明申请

US20120245351A1 PROCESS FOR THE PREPARATION OF LAPATINIB AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS 审中-公开
标题翻译：制备LAPATINIB及其药物接受口服的方法
公开(公告)号：US20120245351A1
公开(公告)日：2012-09-27
申请号：US13498389
申请日：2009-09-29
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： C07D239/94
CPC分类号： C07D405/04
摘要： The present invention relates to an improved and new 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-quip-azolinamine and its pharmaceutically acceptable salts.
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（R））的式（1）的拉帕替尼的高纯度晶体碱的改进和新方法 - （{[2-（甲磺酰基）乙基]氨基}甲基] -2-呋喃基] -4-哒唑啉胺及其药学上可接受的盐。

8. 发明授权

US09050341B2 Methods of treating drug resistant and other tumors by administering 6,7-dialkoxy quinazoline derivatives 有权
标题翻译：通过施用6,7-二烷氧基喹唑啉衍生物治疗耐药性和其它肿瘤的方法
公开(公告)号：US09050341B2
公开(公告)日：2015-06-09
申请号：US12833733
申请日：2010-07-09
申请人： Bhujanga rao Abidhatla Kali Satya , Ramanadham Jyothi Prasad , Bollepalli Nageshwara Rao , Nannapaneni Venkaiah Chowdary
发明人： Bhujanga rao Abidhatla Kali Satya , Ramanadham Jyothi Prasad , Bollepalli Nageshwara Rao , Nannapaneni Venkaiah Chowdary
IPC分类号： A61K31/535 , A61K31/497 , A61K31/517
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。

9. 发明授权

US08921362B2 6,7-dialkoxy quinazoline derivatives and methods of treating drug resistant and other tumors 有权
标题翻译： 6,7-二烷氧基喹唑啉衍生物和治疗耐药性等肿瘤的方法
公开(公告)号：US08921362B2
公开(公告)日：2014-12-30
申请号：US12833789
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： A61K31/535 , A61K31/497 , C07D239/94
CPC分类号： A61K31/5377 , C07D239/94
摘要： Compounds of formula (I) in which: R1 is: R2 is —CH3 or —CH2CH3; or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions including the compound of formula (I) and a pharmaceutically acceptable carrier. Processes for preparing the compound of formula (I). Methods of inhibiting a receptor tyrosine kinase in a subject in need thereof. Methods of inhibiting the growth of a tumor cell in a subject in need thereof. Methods of treating pancreatic cancer in a subject in need of treatment for pancreatic cancer. Methods of treating HER2 positive breast cancer in a subject in need of treatment for HER2 positive breast cancer. Methods of 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.
摘要翻译：式（I）化合物，其中：R1为：R2为-CH3或-CH2CH3; 或其药学上可接受的盐。药物组合物，包括式（I）化合物和药学上可接受的载体。制备式（I）化合物的方法。在有需要的受试者中抑制受体酪氨酸激酶的方法。抑制有需要的受试者中肿瘤细胞生长的方法。在需要胰腺癌治疗的受试者中治疗胰腺癌的方法。在需要治疗HER2阳性乳腺癌的个体中治疗HER2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治疗耐药性非小细胞肺癌的方法。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。

10. 发明授权

US08143250B2 6-7,dialkoxy quinazoline derivatives useful for treatment of cancer related disorders 有权
标题翻译： 6-7，可用于治疗癌症相关疾病的二烷氧基喹唑啉衍生物
公开(公告)号：US08143250B2
公开(公告)日：2012-03-27
申请号：US12812726
申请日：2008-01-18
申请人： Ramanadham Jyothi Prasad , Bhujanga Rao Adibhatla Kali Satya , Bollepalli Nageshwara Rao , Nannapaneni Venkaiah Chowdary
发明人： Ramanadham Jyothi Prasad , Bhujanga Rao Adibhatla Kali Satya , Bollepalli Nageshwara Rao , Nannapaneni Venkaiah Chowdary
IPC分类号： A61K31/5377 , C07D413/12 , A61P35/00
CPC分类号： A61K31/5377 , C07D239/94
摘要： In view of the great potential the quinazoline class of compounds offer, we started the synthesis and screening of a large number of new chemical entities with novel structural features. It has been surprisingly and unexpectedly found that quinazolines having 3-Ethynyl anilino group at the 4th position and specifically substituted alkoxy groups in the 6 and 7 positions, impart much enhanced and special anti-proliferative properties when compared to other prominent members of the quinazoline class of drugs. Also, surprisingly the compounds of this invention are much less toxic and the safety profile is exceedingly beneficial for therapeutic applications. The novel chemical entities described in this invention are designated by the general structure (I) and have not been synthesized earlier nor investigated for their therapeutic benefits and safety profile. Compound (I) is NRC-2694, when structure (A).
摘要翻译：鉴于喹唑啉类化合物具有巨大的潜力，我们开始对大量具有新型结构特征的新化学物质进行合成和筛选。出人意料地发现，与喹唑啉类的其他显着成分相比，在第4位具有3-乙炔基苯胺基的6和7位上具有特异性取代的烷氧基的喹唑啉具有很强的增强和特殊的抗增殖特性的药物。此外，令人惊讶的是，本发明的化合物毒性远低于安全性，对于治疗应用是非常有益的。本发明中描述的新颖化学实体由通式结构（I）表示，并没有早期合成，也没有对其治疗益处和安全性进行调查。当结构（A）时，化合物（I）是NRC-2694。

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