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1. 发明授权

US07524837B2 Benzotriazapinone salts and methods for using same 有权
标题翻译：苯并三氮杂酮盐及其使用方法
公开(公告)号：US07524837B2
公开(公告)日：2009-04-28
申请号：US10833232
申请日：2004-04-27
申请人： Ahmed F. Abdel-Magid , Judith H. Cohen
发明人： Ahmed F. Abdel-Magid , Judith H. Cohen
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D255/04 , C07D401/12 , C07D403/12 , C07D403/14 , C07D405/06 , C07D405/12 , C07D409/12 , C07D413/06 , C07D413/12 , C07D417/12
摘要： This invention relates to pharmaceutically acceptable salts of compounds of formula (I) Such salts are useful, for example, for the treatment of gastrin related disorders.
摘要翻译：本发明涉及式（I）化合物的药学上可接受的盐。这种盐可用于例如治疗胃泌素相关疾病。

2. 发明授权

US06610855B2 Synthesis of 3-amino-3-aryl propanoates 有权
标题翻译： 3-氨基-3-芳基丙酸酯的合成
公开(公告)号：US06610855B2
公开(公告)日：2003-08-26
申请号：US10197286
申请日：2002-07-15
申请人： Ahmed F. Abdel-Magid , Judith H. Cohen , Cynthia A. Maryanoff , Frank John Villani, Jr. , Hua M. Zhong
发明人： Ahmed F. Abdel-Magid , Judith H. Cohen , Cynthia A. Maryanoff , Frank John Villani, Jr. , Hua M. Zhong
IPC分类号： C07D21355
CPC分类号： C07C227/32 , C07B2200/07 , C07C229/34
摘要： A process for the synthesis of a compound of the formula wherein R1 is aryl, heteroaryl, substituted aryl or substituted heteroaryl and R2 is hydrogen, alkyl or aralkyl, or salt thereof.
摘要翻译：用于合成糠醛的化合物R 1的方法是芳基，杂芳基，取代的芳基或取代的杂芳基，R 2是氢，烷基或芳烷基或其盐。

3. 发明授权

US4894374A Substituted 1,2-dihydro-4h-3,1-benzoxazin-4-one derivatives inhibitors of interleukin 1 失效
标题翻译：取代的1,2-二氢-4h-3,1-苯并恶嗪-4-酮衍生物白细胞介素1抑制剂
公开(公告)号：US4894374A
公开(公告)日：1990-01-16
申请号：US233186
申请日：1988-08-17
申请人： Jerauld S. Skotnicki , Ahmed F. Abdel-Magid
发明人： Jerauld S. Skotnicki , Ahmed F. Abdel-Magid
IPC分类号： A61K31/535 , C07D498/10
CPC分类号： C07D498/10 , A61K31/535
摘要： There are disclosed compounds of the formula: ##STR1## wherein X is CHR, NR.sup.1, S or O;R is hydrogen, lower alkenyl, pyridyl, quinolinyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, or substituted phenyl, naphthyl, pyridyl, quinolinyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, wherein the substituents are selected from halo, carboxy, lower alkoxycarbonyl, lower alkylsulfonyl, cyano, nitro and trifluoromethyl;R.sup.1 is lower alkenyl, pyridyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, or substituted phenyl, naphthyl, pyridyl, quinolinyl, pyrazinyl, pyrimidinyl, quinoxalinyl or quinazolinyl, wherein the substituents are selected from halo, carboxy, lower alkoxycarbonyl, lower alkylsulfonyl, cyano, nitro and trifluoromethyl; andR.sup.2 and R.sup.3 are each, independently, hydrogen, halo, lower alkyl, lower alkenyl, lower alkoxy, hydroxy, amino, mono- or diloweralkylamino, carboxy, lower alkoxycarbonyl, nitro or cyano;which, by virtue of their ability to inhibit interleukin 1, are of use as antiinflammatory agents and in treatment of disease states involving enzymatic tissue destruction, and there is also disclosed a method using such compounds in the treatment of immunoinflammatory, inflammatory/proliferative and enzymatic tissue destruction conditions.
摘要翻译：公开了下式的化合物：其中X是CHR，NR1，S或O; 吡啶基，喹喔啉基或喹唑啉基，或取代的苯基，萘基，吡啶基，喹啉基，吡嗪基，嘧啶基，喹喔啉基或喹唑啉基，其中取代基选自卤素，羧基，低级烷氧基羰基，低级烷基磺酰基，氰基，硝基和三氟甲基; R 1是低级烯基，吡啶基，吡嗪基，嘧啶基，喹喔啉基或喹唑啉基，或取代的苯基，萘基，吡啶基，喹啉基，吡嗪基，嘧啶基，喹喔啉基或喹唑啉基，其中取代基选自卤素，羧基，低级烷氧基羰基，低级烷基磺酰基，，硝基和三氟甲基; 卤素，低级烷基，低级烯基，低级烷氧基，羟基，氨基，单 - 或二 - 低级烷基氨基，羧基，低级烷氧羰基，硝基或氰基; 由于其抑制白细胞介素1的能力，可用作抗炎剂和治疗涉及酶组织破坏的疾病状态，并且还公开了使用这些化合物治疗免疫炎症，炎症/增殖和酶促的方法组织破坏条件。

4. 发明申请

US20090233874A1 PROCESS FOR THE PREPARATION OF COMPOUNDS USEFUL AS INHIBITORS OF SGLT 有权
标题翻译：制备作为SGLT抑制剂的化合物的方法
公开(公告)号：US20090233874A1
公开(公告)日：2009-09-17
申请号：US12207252
申请日：2008-09-09
申请人： Ahmed F. Abdel-Magid , Maureen Chisholm , Steven Mehrman , Lorraine Scott , Kenneth M. Wells , Fan Zhang-Plasket , Sumihiro Nomura , Mitsuya Hongu , Yuichi Koga
发明人： Ahmed F. Abdel-Magid , Maureen Chisholm , Steven Mehrman , Lorraine Scott , Kenneth M. Wells , Fan Zhang-Plasket , Sumihiro Nomura , Mitsuya Hongu , Yuichi Koga
IPC分类号： A61K31/706 , C07H7/06 , A61P3/10
CPC分类号： C07D409/10 , C07D309/10 , C07D309/12 , C07D409/14 , C07D417/14
摘要： The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.
摘要翻译：本发明涉及一种制备具有抑制活性的化合物的新方法，所述化合物对存在于肠或肾中的钠依赖性葡萄糖转运蛋白（SGLT）具有抑制活性。

5. 发明授权

US06613914B2 Process for preparing 1, 5-diaryl-3-substituted pyrazoles 有权
标题翻译：制备1,5-二芳基-3-取代的吡唑的方法
公开(公告)号：US06613914B2
公开(公告)日：2003-09-02
申请号：US10086583
申请日：2002-03-01
申请人： Ahmed F. Abdel-Magid , Bruce D. Harris , Cynthia A. Maryanoff
发明人： Ahmed F. Abdel-Magid , Bruce D. Harris , Cynthia A. Maryanoff
IPC分类号： C07D23112
CPC分类号： C07D231/12 , C07C51/083 , C07C59/88
摘要： A process for making a compound of formula I wherein the substituents are as described in the specification comprising reacting a ketone of formula II with succinic anhydride and an alkoxide base to form a compound of formula III which is reacted with a compound of formula IV to form a compound of V and reacting with an alcohol to form the corresponding ester of formula VI and reacting the ester with N-methylhydroxylamine.
摘要翻译：制备式I化合物的方法，其中取代基如说明书中所述包括使式II的酮与琥珀酸酐和醇盐碱反应形成式III化合物，其与式IV化合物反应形成钒的化合物与醇反应以形成相应的式VI的酯，并使酯与N-甲基羟胺反应。

6. 发明授权

US6013764A Liquid phase peptide synthesis of KL-4 pulmonary surfactant 失效
标题翻译： KL-4肺表面活性剂的液相肽合成
公开(公告)号：US6013764A
公开(公告)日：2000-01-11
申请号：US881971
申请日：1997-06-25
申请人： Ahmed F. Abdel-Magid , Urs Eggmann , Cynthia Anne Maryanoff , Adrian Thaler , Frank J. Villani
发明人： Ahmed F. Abdel-Magid , Urs Eggmann , Cynthia Anne Maryanoff , Adrian Thaler , Frank J. Villani
IPC分类号： A61K38/00 , C07K1/12 , C07K5/083 , C07K5/09 , C07K14/785 , C07K1/02 , C07K1/08 , C07K1/10 , C07K14/00
CPC分类号： C07K5/0808 , C07K1/126 , C07K14/785 , C07K5/0815 , A61K38/00
摘要： The invention relates to improved liquid phase processes for the preparation of the 21 residue protein component, (Lys-Leu.sub.4).sub.4 -Lys, of the pulmonary surfactant KL-4. These process are amenable to large scale synthesis and one process employs a method of saponifying an ester which reduces the inherent racemization of the .alpha.-carbon.
摘要翻译：本发明涉及用于制备肺表面活性剂KL-4的21个残基蛋白组分（Lys-Leu4）4-Lys的改进的液相方法。这些方法适合于大规模合成，一种方法采用皂化方法来降低α-碳的固有外消旋化。

7. 发明授权

US08669288B2 Lysine salts of 4-((phenoxyalkyl)thio)-phenoxyacetic acid derivatives 有权
标题翻译： 4 - （（苯氧基烷基）硫代） - 苯氧基乙酸衍生物的赖氨酸盐
公开(公告)号：US08669288B2
公开(公告)日：2014-03-11
申请号：US12726457
申请日：2010-03-18
申请人： Ahmed F. Abdel-Magid , Steven J. Mehrman , Armin Roessler
发明人： Ahmed F. Abdel-Magid , Steven J. Mehrman , Armin Roessler
IPC分类号： A61K31/205 , C07C323/22
CPC分类号： C07C323/20
摘要： The present invention is directed to a novel lysine salts, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by PPAR delta. The present invention is further directed to a novel process for the preparation of said lysine salts.
摘要翻译：本发明涉及含有它们的新型赖氨酸盐，药物组合物及其用于治疗由PPARδ调节的病症和状况的用途。本发明进一步涉及制备所述赖氨酸盐的新方法。

8. 发明申请

US20090259021A1 Liquid Phase Peptide Synthesis of KL-4 Pulmonary Surfactant 有权
标题翻译： KL-4肺表面活性剂的液相肽合成
公开(公告)号：US20090259021A1
公开(公告)日：2009-10-15
申请号：US12241171
申请日：2008-09-30
申请人： Ahmed F. Abdel-Magid , Urs Eggmann , Cynthia Anne Maryanoff , Adrian Thaler , Frank J. Villani
发明人： Ahmed F. Abdel-Magid , Urs Eggmann , Cynthia Anne Maryanoff , Adrian Thaler , Frank J. Villani
IPC分类号： C07K1/06
CPC分类号： C07K5/0808 , A61K38/00 , C07K1/126 , C07K5/0815 , C07K14/785
摘要： The invention relates to improved liquid phase processes for the preparation of the 21 residue protein component, (Lys-Leu4)4-Lys, of the pulmonary surfactant KL-4. These process are amenable to large scale synthesis and one process employs a method of saponifying an ester which reduces the inherent racemization of the α-carbon.
摘要翻译：本发明涉及用于制备肺表面活性剂KL-4的21个残基蛋白组分（Lys-Leu4）4-Lys的改进的液相方法。这些方法适合于大规模合成，一种方法采用皂化方法来降低α-碳的固有外消旋化。

9. 发明授权

US07247745B2 Process for preparing 1,5-diaryl-3-substituted pyrazoles 有权
标题翻译：制备1,5-二芳基-3-取代的吡唑的方法
公开(公告)号：US07247745B2
公开(公告)日：2007-07-24
申请号：US11215329
申请日：2005-08-30
申请人： Ahmed F. Abdel-Magid , Bruce D. Harris , Cynthia A. Maryanoff
发明人： Ahmed F. Abdel-Magid , Bruce D. Harris , Cynthia A. Maryanoff
IPC分类号： C07C61/00
CPC分类号： C07D231/12 , C07C51/083 , C07C59/88
摘要： A process for making a compound of formula I wherein the substituents are as described in the specification comprising reacting a ketone of formula II with succinic anhydride and an alkoxide base to form a compound of formula III which is reacted with a compound of formula IV to form a compound of V and reacting with an alcohol to form the corresponding ester of formula VI and reacting the ester with N-methylhydroxylamine.
摘要翻译：制备式I化合物的方法，其中取代基如说明书中所述包括使式II的酮与琥珀酸酐和醇盐碱反应形成式III化合物，其与式IV化合物反应形成 V的化合物并与醇反应以形成相应的式VI的酯并使酯与N-甲基羟胺反应。

10. 发明授权

US06953860B2 Process for preparing 1,5-diaryl-3-substituted pyrazoles 有权
标题翻译：制备1,5-二芳基-3-取代的吡唑的方法
公开(公告)号：US06953860B2
公开(公告)日：2005-10-11
申请号：US10460601
申请日：2003-06-12
申请人： Ahmed F. Abdel-Magid , Bruce D. Harris , Cynthia A. Maryanoff
发明人： Ahmed F. Abdel-Magid , Bruce D. Harris , Cynthia A. Maryanoff
IPC分类号： C07C51/083 , C07C59/86 , C07C59/88 , C07D231/12 , A61K31/415
CPC分类号： C07D231/12 , C07C51/083 , C07C59/88
摘要： A process for making a compound of formula I wherein the substituents are as described in the specification comprising reacting a ketone of formula II with succinic anhydride and an alkoxide base to form a compound of formula III which is reacted with a compound of formula IV to form a compound of V and reacting with an alcohol to form the corresponding ester of formula VI and reacting the ester with N-methylhydroxylamine.
摘要翻译：制备式I化合物的方法，其中取代基如说明书中所述包括使式II的酮与琥珀酸酐和醇盐碱反应形成式III化合物，其与式IV化合物反应形成 V的化合物并与醇反应以形成相应的式VI的酯并使酯与N-甲基羟胺反应。

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