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1. 发明申请

US20100204505A1 METHODS FOR PRODUCING PHENYLALANINE DERIVATIVES HAVING A QUINAZOLINEDIONE SKELETON AND INTERMEDIATES FOR PRODUCTION THEREOF 有权
标题翻译：用于生产具有四氮唑烷酮的苯乙烯胺衍生物的方法及其生产中间体
公开(公告)号：US20100204505A1
公开(公告)日：2010-08-12
申请号：US12766178
申请日：2010-04-23
申请人： Noriyasu Kataoka , Akinori Tatara , Masanobu Yatagai , Junko Yamanaka
发明人： Noriyasu Kataoka , Akinori Tatara , Masanobu Yatagai , Junko Yamanaka
IPC分类号： C07C229/52
CPC分类号： C07D239/96 , C07C233/87
摘要： The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of reacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s); making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); and N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having α 4 integrin inhibiting activity. In the formulae (1) and (5), R1 represents a phenyl group having a substituent(s) and the like, R2 represents an alkyl group and the like, R3 represents a dialkylamino group and the like, and R4 represents an alkyl group and the like.
摘要翻译：本发明提供了具有式（5）喹唑啉二酮环的苯丙氨酸衍生物的制备方法，包括使式（1）的酰基苯丙氨酸衍生物与羰基引入试剂反应的步骤，和邻氨基苯甲酸的衍生物以形成不对称脲中间体; 在碱的存在下使不对称脲中间体转化为式（4）的喹唑啉二酮化合物; 和得到的喹唑啉二酮化合物的N-烷基化喹唑啉二酮环酰胺与N-烷基化剂。该制造方法是用于生产具有喹唑啉二酮骨架的苯丙氨酸衍生物的工业上适用的方法，其是作为具有α4整联蛋白抑制活性的药物高度有用的化合物。在式（1）和（5）中，R 1表示具有取代基等的苯基，R 2表示烷基等，R 3表示二烷基氨基等，R 4表示烷基等等。

2. 发明授权

US08058432B2 Method for preparing phenylalanine derivatives having quinazoline-dione skeleton and intermediates for use in the preparation of derivatives 有权
标题翻译：制备具有喹唑啉二酮骨架的苯丙氨酸衍生物的方法和用于制备衍生物的中间体
公开(公告)号：US08058432B2
公开(公告)日：2011-11-15
申请号：US12470846
申请日：2009-05-22
申请人： Noriyasu Kataoka , Kotaro Okado , Tatsuhiro Yamada , Koichi Fujita , Tamotsu Suzuki , Tatsuya Okuzumi , Masayuki Sugiki , Akinori Tatara
发明人： Noriyasu Kataoka , Kotaro Okado , Tatsuhiro Yamada , Koichi Fujita , Tamotsu Suzuki , Tatsuya Okuzumi , Masayuki Sugiki , Akinori Tatara
IPC分类号： C07D239/96
CPC分类号： C07D239/96 , C07C233/47 , C07C233/87 , C07C237/40 , C07C237/42 , C07C265/12 , C07C271/22 , C07C271/28 , C07C275/42 , Y02P20/55
摘要： The present invention releates to a method for preparing a phenylalanine compound having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof: where R1-R4 are defined herein. The method involves reacting a specified acyl phenylalanine compound with a carbonyl group-introducing reagent and a specified anthranilic acid compound to form a carboxy-asymmetric urea compound which is converted to a quinazoline-dione compound in the presence of a carboxyl group-activating agent.
摘要翻译：本发明涉及制备具有由下式（1）表示的喹唑啉二酮环的苯丙氨酸化合物或其药学上可接受的盐的方法：其中R1-R4如本文所定义。该方法包括使特定的酰基苯丙氨酸化合物与羰基引入试剂和特定的邻氨基苯甲酸化合物反应，形成羧基不对称脲化合物，其在羧基活化剂存在下转化为喹唑啉二酮化合物。

3. 发明授权

US07951942B2 Crystals of phenylalanine derivatives and production methods thereof 有权
标题翻译：苯丙氨酸衍生物的晶体及其制备方法
公开(公告)号：US07951942B2
公开(公告)日：2011-05-31
申请号：US12697816
申请日：2010-02-01
申请人： Shinichiro Takahashi , Noriyasu Kataoka , Akinori Tatara , Toshihiro Matsuzawa
发明人： Shinichiro Takahashi , Noriyasu Kataoka , Akinori Tatara , Toshihiro Matsuzawa
IPC分类号： C07D239/72
CPC分类号： C07D239/96
摘要： The present invention provides crystals of phenylalanine derivatives of the formula (I): and particularly α-type, γ-type, ε-type, η-type, and θ-type crystals thereof. These crystals are excellent in preservation stability or moisture resistance. They can also be produced on an industrial scale.
摘要翻译：本发明提供式（I）的苯丙氨酸衍生物的晶体，特别是α型，γ型，类型，类型和类型的晶体。这些晶体的保存稳定性或耐湿性优异。它们也可以在工业规模生产。

4. 发明申请

US20100137593A1 CRYSTALS OF PHENYLALANINE DERIVATIVES AND PRODUCTION METHODS THEREOF 有权
标题翻译：苯乙烯衍生物的结晶及其生产方法
公开(公告)号：US20100137593A1
公开(公告)日：2010-06-03
申请号：US12697816
申请日：2010-02-01
申请人： Shinichiro Takahashi , Noriyasu Kataoka , Akinori Tatara , Toshihiro Matsuzawa
发明人： Shinichiro Takahashi , Noriyasu Kataoka , Akinori Tatara , Toshihiro Matsuzawa
IPC分类号： C07D239/96
CPC分类号： C07D239/96
摘要： The present invention provides crystals of phenylalanine derivatives of the formula (I): and particularly α-type, γ-type, ε-type, η-type, and θ-type crystals thereof. These crystals are excellent in preservation stability or moisture resistance. They can also be produced on an industrial scale.
摘要翻译：本发明提供式（I）的苯丙氨酸衍生物的晶体，特别是α型，γ型，类型，类型和类型的晶体。这些晶体的保存稳定性或耐湿性优异。它们也可以在工业规模生产。

5. 发明申请

US20110313154A1 METHOD FOR PREPARING PHENYLALANINE DERIVATIVES HAVING QUINAZOLINE-DIONE SKELETON AND INTERMEDIATES FOR USE IN THE PREPARATION OF THE DERIVATIVES 有权
标题翻译：制备具有喹唑啉酮骨架的苯乙烯胺衍生物的方法和用于制备衍生物的中间体
公开(公告)号：US20110313154A1
公开(公告)日：2011-12-22
申请号：US13218946
申请日：2011-08-26
申请人： Noriyasu KATAOKA , Kotaro OKADO , Tatsuhiro YAMADA , Koichi FUJITA , Tamotsu SUZUKI , Tatsuya OKUZUMI , Masayuki SUGIKI , Akinori TATARA
发明人： Noriyasu KATAOKA , Kotaro OKADO , Tatsuhiro YAMADA , Koichi FUJITA , Tamotsu SUZUKI , Tatsuya OKUZUMI , Masayuki SUGIKI , Akinori TATARA
IPC分类号： C07C229/66 , C07C229/42 , C07D265/26 , C07C229/52 , C07C229/38 , C07C271/22 , C07D239/96
CPC分类号： C07D239/96 , C07C233/47 , C07C233/87 , C07C237/40 , C07C237/42 , C07C265/12 , C07C271/22 , C07C271/28 , C07C275/42 , Y02P20/55
摘要： A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3′ which is a group corresponding to R3 is protected. According to this method, there can be obtained a phenylalanine derivative having a quinazoline-dione skeleton in a industrially favorably high yield.
摘要翻译：一种制备具有由下式（1）表示的喹唑啉二酮环的苯丙氨酸衍生物或其药学上可接受的盐的方法，包括以下步骤（a），（b）和（c）：（a）使酰基由下式（2）表示的苯丙氨酸衍生物：具有羰基导入试剂和特定的邻氨基苯甲酸衍生物，从而形成相应的羧基不对称脲衍生物; （b）在羧基活化剂存在下将羧基不对称脲衍生物转化为相应的喹唑啉二酮衍生物：（c）如果需要，用N-烷基取代与氮原子键合的氢原子存在在使用N-烷基化试剂的喹唑啉二酮衍生物的喹唑啉二酮环中，然后当对应于R3的基团的取代基R3'被保护时，使得到的产物脱保护。根据该方法，可以得到具有喹唑啉二酮骨架的苯丙氨酸衍生物，工业上有利地高产率。

6. 发明授权

US07683169B2 Crystals of phenylalanine derivatives and production methods thereof 有权
标题翻译：苯丙氨酸衍生物的晶体及其制备方法
公开(公告)号：US07683169B2
公开(公告)日：2010-03-23
申请号：US11441106
申请日：2006-05-26
申请人： Shinichiro Takahashi , Noriyasu Kataoka , Akinori Tatara , Toshihiro Matsuzawa
发明人： Shinichiro Takahashi , Noriyasu Kataoka , Akinori Tatara , Toshihiro Matsuzawa
IPC分类号： C07D239/72
CPC分类号： C07D239/96
摘要： The present invention provides crystals of phenylalanine derivatives of the formula (I): and particularly α-type, γ-type, ε-type, η-type, and θ-type crystals thereof. These crystals are excellent in preservation stability or moisture resistance. They can also be produced on an industrial scale.
摘要翻译：本发明提供式（I）的苯丙氨酸衍生物的晶体，特别是α型，γ型，类型，类型和类型的晶体。这些晶体的保存稳定性或耐湿性优异。它们也可以在工业规模生产。

7. 发明申请

US20070018172A1 Crystals of phenylalanine derivatives and production methods thereof 有权
标题翻译：苯丙氨酸衍生物的晶体及其制备方法
公开(公告)号：US20070018172A1
公开(公告)日：2007-01-25
申请号：US11441106
申请日：2006-05-26
申请人： Shinichiro Takahashi , Noriyasu Kataoka , Akinori Tatara , Toshihiro Matsuzawa
发明人： Shinichiro Takahashi , Noriyasu Kataoka , Akinori Tatara , Toshihiro Matsuzawa
IPC分类号： H01L29/15
CPC分类号： C07D239/96
摘要： The present invention provides crystals of phenylalanine derivatives of the formula (I): and particularly α-type, γ-type, ∈-type, η-type, and θ-type crystals thereof. These crystals are excellent in preservation stability or moisture resistance. They can also be produced on an industrial scale.
摘要翻译：本发明提供式（I）的苯丙氨酸衍生物的晶体，特别是α型，γ型，ε型，eta型和θ型晶体。这些晶体的保存稳定性或耐湿性优异。它们也可以在工业规模生产。

8. 发明授权

US08546610B2 Method for preparing phenylalanine derivatives having quinazoline-dione skeleton and intermediates for use in the preparation of the derivatives 有权
标题翻译：制备具有喹唑啉二酮骨架的苯丙氨酸衍生物的方法和用于制备衍生物的中间体
公开(公告)号：US08546610B2
公开(公告)日：2013-10-01
申请号：US13218946
申请日：2011-08-26
申请人： Noriyasu Kataoka , Kotaro Okado , Tatsuhiro Yamada , Koichi Fujita , Tamotsu Suzuki , Tatsuya Okuzumi , Masayuki Sugiki , Akinori Tatara
发明人： Noriyasu Kataoka , Kotaro Okado , Tatsuhiro Yamada , Koichi Fujita , Tamotsu Suzuki , Tatsuya Okuzumi , Masayuki Sugiki , Akinori Tatara
IPC分类号： C07C229/56
CPC分类号： C07D239/96 , C07C233/47 , C07C233/87 , C07C237/40 , C07C237/42 , C07C265/12 , C07C271/22 , C07C271/28 , C07C275/42 , Y02P20/55
摘要： A method for preparing a phenylalanine derivative having a quinazoline-dione ring represented by the following formula (1) or a pharmaceutically acceptable salt thereof, comprising the following steps (a), (b) and (c): (a) reacting an acyl phenylalanine derivative represented by the following formula (2): with a carbonyl group-introducing reagent and a specific anthranilic acid derivative to thus form the corresponding carboxy-asymmetric urea derivative; (b) converting the carboxy-asymmetric urea derivative into the corresponding quinazoline-dione derivative in the presence of a carboxyl group-activating agent: (c) if desired, substituting an N-alkyl group for the hydrogen atom bonded to the nitrogen atom present in the quinazoline-dione ring of the quinazoline-dione derivative using an N-alkylation agent and then deprotecting the resulting product, when the substituent R3′ which is a group corresponding to R3 is protected. According to this method, there can be obtained a phenylalanine derivative having a quinazoline-dione skeleton in a industrially favorably high yield.
摘要翻译：一种制备具有由下式（1）表示的喹唑啉二酮环的苯丙氨酸衍生物或其药学上可接受的盐的方法，包括以下步骤（a），（b）和（c）：（a）使酰基由下式（2）表示的苯丙氨酸衍生物：具有羰基导入试剂和特定的邻氨基苯甲酸衍生物，从而形成相应的羧基不对称脲衍生物; （b）在羧基活化剂存在下将羧基不对称脲衍生物转化为相应的喹唑啉二酮衍生物：（c）如果需要，用N-烷基取代与氮原子键合的氢原子存在在使用N-烷基化试剂的喹唑啉二酮衍生物的喹唑啉二酮环中，然后当对应于R3的基团的取代基R3'被保护时，使得到的产物脱保护。根据该方法，可以得到具有喹唑啉二酮骨架的苯丙氨酸衍生物，工业上有利地高产率。

9. 发明授权

US08318975B2 Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof 有权
标题翻译：具有喹唑啉二酮骨架的苯丙氨酸衍生物的制造方法及其制造用中间体
公开(公告)号：US08318975B2
公开(公告)日：2012-11-27
申请号：US12766178
申请日：2010-04-23
申请人： Noriyasu Kataoka , Akinori Tatara , Masanobu Yatagai , Junko Yamanaka
发明人： Noriyasu Kataoka , Akinori Tatara , Masanobu Yatagai , Junko Yamanaka
IPC分类号： C07C63/04
CPC分类号： C07D239/96 , C07C233/87
摘要： The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of reacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s); making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); and N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having α 4 integrin inhibiting activity. In the formulae (1) and (5), R1 represents a phenyl group having a substituent(s) and the like, R2 represents an alkyl group and the like, R3 represents a dialkylamino group and the like, and R4 represents an alkyl group and the like.
摘要翻译：本发明提供了具有式（5）喹唑啉二酮环的苯丙氨酸衍生物的制备方法，包括使式（1）的酰基苯丙氨酸衍生物与羰基引入试剂反应的步骤，和邻氨基苯甲酸的衍生物以形成不对称脲中间体; 在碱的存在下使不对称脲中间体转化为式（4）的喹唑啉二酮化合物; 和得到的喹唑啉二酮化合物的N-烷基化喹唑啉二酮环酰胺与N-烷基化剂。该制造方法是用于生产具有喹唑啉二酮骨架的苯丙氨酸衍生物的工业上适用的方法，其是作为具有α4整联蛋白抑制活性的药物高度有用的化合物。在式（1）和（5）中，R 1表示具有取代基等的苯基，R 2表示烷基等，R 3表示二烷基氨基等，R 4表示烷基等等。

10. 发明授权

US07737274B2 Methods for producing phenylalanine derivatives having a quinazolinedione skeleton and intermediates for production thereof 有权
标题翻译：具有喹唑啉二酮骨架的苯丙氨酸衍生物的制造方法及其制造用中间体
公开(公告)号：US07737274B2
公开(公告)日：2010-06-15
申请号：US11207751
申请日：2005-08-22
申请人： Noriyasu Kataoka , Akinori Tatara , Masanobu Yatagai , Junko Yamanaka
发明人： Noriyasu Kataoka , Akinori Tatara , Masanobu Yatagai , Junko Yamanaka
IPC分类号： A61K31/517 , C07D239/80 , C07D239/88 , C07C61/08 , C07C63/06 , C07C229/56
CPC分类号： C07D239/96 , C07C233/87
摘要： The present invention provides a method for producing a phenylalanine derivative(s) having a quinazolinedione ring of formula (5), including steps comprising of reacting an acylphenylalanine derivative(s) of formula (1) with a carbonyl group-introducing reagent(s) and a derivative(s) of anthranilic acid to form an asymmetric urea intermediate(s); making the asymmetric urea intermediate(s) into a quinazolinedione compound(s) of formula (4) in the presence of a base(s); and N-alkylating quinazolinedione ring amide of the obtained quinazolinedione compounds with N-alkylation agents. This production method is an industrially applicable method for producing phenylalanine derivatives having a quinazolinedione skeleton, which are compounds highly useful as drugs having α 4 integrin inhibiting activity. In the formulae (1) and (5), R1 represents a phenyl group having a substituent(s) and the like, R2 represents an alkyl group and the like, R3 represents a dialkylamino group and the like, and R4 represents an alkyl group and the like.
摘要翻译：本发明提供了具有式（5）喹唑啉二酮环的苯丙氨酸衍生物的制备方法，包括使式（1）的酰基苯丙氨酸衍生物与羰基引入试剂反应的步骤，和邻氨基苯甲酸的衍生物以形成不对称脲中间体; 在碱的存在下使不对称脲中间体转化为式（4）的喹唑啉二酮化合物; 和得到的喹唑啉二酮化合物的N-烷基化喹唑啉二酮环酰胺与N-烷基化剂。该制造方法是用于生产具有喹唑啉二酮骨架的苯丙氨酸衍生物的工业上适用的方法，其是作为具有α4整联蛋白抑制活性的药物高度有用的化合物。在式（1）和（5）中，R 1表示具有取代基等的苯基，R 2表示烷基等，R 3表示二烷基氨基等，R 4表示烷基等等。

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