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1. 发明授权

US06268535B1 Synthesis of 3-aryl-1-indanamines 失效
标题翻译： 3-芳基-1-茚满胺的合成
公开(公告)号：US06268535B1
公开(公告)日：2001-07-31
申请号：US09226469
申请日：1999-01-07
申请人： Adel M. Moussa , Reem Haider , Heather Taft , Jurjus Jurayj , Weiheng Wang , HaeSuk Suh
发明人： Adel M. Moussa , Reem Haider , Heather Taft , Jurjus Jurayj , Weiheng Wang , HaeSuk Suh
IPC分类号： C07C21100
CPC分类号： C07C209/16 , C07B2200/09 , C07C29/143 , C07C45/46 , C07C51/353 , C07C2602/08 , C12C11/02 , C07C49/697 , C07C57/58 , C07C211/42 , C07C35/32 , C07C35/52
摘要： The present invention is a method of preparing a 3-aryl-1-indanamine represented by structural formula I: and physiologically acceptable salts thereof. In structure I, phenyl ring A can be unsubstituted or substituted with 1-4 substitutents. R1 is an aromatic group which can be substituted or unsubstituted. R2 and R3 are each, independently, hydrogen, an aliphantic group, a substituted aliphatic group, an aromatic group, a substituted aromatic group, an aralkyl group, or a substituted aralkyl group. Alternatively, R2 and R3, taken together with the nitrogen substitutent on the indan ring, form a non-aromatic ring system having 1-2 heteroatoms.
摘要翻译：本发明是制备由结构式I表示的3-芳基-1-茚满胺及其生理上可接受的盐的方法。在结构I中，苯环A可以是未取代的或被1-4个取代基取代.R1是芳香族可以被取代或未取代的基团.R 2和R 3各自独立地为氢，芳族基团，取代的脂族基团，芳族基团，取代的芳族基团，芳烷基或取代的芳烷基。或者，R 2和R 3与茚满环上的氮取代基一起形成具有1-2个杂原子的非芳族环系。

2. 发明授权

US06462221B1 Synthesis of nitroalcohol diastereomers 失效
标题翻译：硝基醇非对映异构体的合成
公开(公告)号：US06462221B1
公开(公告)日：2002-10-08
申请号：US09574620
申请日：2000-05-19
申请人： Richard L. Gabriel , Adel M. Moussa , Sharon Fitzhenry , Changhua Liu , David A. Swanson , Brittany La , Salah Zahr , Yesh P. Sachdeva , Jurjus Jurayj
发明人： Richard L. Gabriel , Adel M. Moussa , Sharon Fitzhenry , Changhua Liu , David A. Swanson , Brittany La , Salah Zahr , Yesh P. Sachdeva , Jurjus Jurayj
IPC分类号： C07C20502
CPC分类号： C07C213/00 , C07B2200/07 , Y02P20/55 , C07C215/08
摘要： The present invention relates to a method of preparing a 1-nitro-3-substituted-3-amino-2-propanol diastereomer represented by Structural Formula I: In Structural Formula I, R is an amine protecting group, and R1 is an amino acid side-chain, a protected amino acid side-chain, a substituted or unsubstituted aliphatic group, a substituted or unsubstituted aromatic group, a substituted or unsubstituted heteroaromatic group, a substituted or unsubstituted aralkyl or a substituted or unsubstituted heteroaralkyl group. The method involves contacting a 1-nitro-3-substituted-3-amino-2-propanone with a reducing agent to form a mixture of 1-nitro-3-substituted-3-amino-2-propanol diastereomers. The 1-nitro-3-substituted-3-amino-2-propanol diastereomers are then separated by simulated moving bed chromatography to obtain one or more 1-nitro-3-substituted-3-amino-2-propanol diastereomer.
摘要翻译：本发明涉及由结构式I表示的1-硝基-3-取代-3-氨基-2-丙醇非对映体的制备方法：在结构式I中，R是胺保护基，R 1是氨基酸取代或未取代的芳族基团，取代或未取代的杂芳族基团，取代或未取代的芳烷基或取代或未取代的杂芳烷基。该方法包括使1-硝基-3-取代-3-氨基-2-丙酮与还原剂接触以形成1-硝基-3-取代-3-氨基-2-丙醇非对映异构体的混合物。然后通过模拟移动床层析分离1-硝基-3-取代-3-氨基-2-丙醇非对映异构体，得到一种或多种1-硝基-3-取代-3-氨基-2-丙醇非对映异构体。

3. 发明授权

US07342038B2 Substituted diphenyl indanone, indane and indole compounds and analogues thereof useful for the treatment or prevention of diseases characterized by abnormal cell proliferation 失效
标题翻译：用于治疗或预防以异常细胞增殖为特征的疾病的取代的二苯基二氢茚酮，二氢化茚和吲哚化合物及其类似物
公开(公告)号：US07342038B2
公开(公告)日：2008-03-11
申请号：US10858975
申请日：2004-06-01
申请人： Carlo Brugnara , Jose Halperin , Rudolf Fluckiger , Emile M. Bellott, Jr. , Richard John Lombardy , John J. Clifford , Ying-Duo Gao , Reem M. Haidar , Eugene W. Kelleher , Adel M. Moussa , Yesh P. Sachdeva , Minghua Sun , Heather N. Taft
发明人： Carlo Brugnara , Jose Halperin , Rudolf Fluckiger , Emile M. Bellott, Jr. , Richard John Lombardy , John J. Clifford , Ying-Duo Gao , Reem M. Haidar , Eugene W. Kelleher , Adel M. Moussa , Yesh P. Sachdeva , Minghua Sun , Heather N. Taft
IPC分类号： C07D209/10 , C07D209/12 , A61K31/404
CPC分类号： C07D317/20 , C07C35/32 , C07C43/188 , C07C43/192 , C07C45/46 , C07C45/68 , C07C235/34 , C07C235/78 , C07C251/44 , C07C255/36 , C07C255/40 , C07C2602/08 , C07D209/40 , C07D303/46 , C07C49/697 , C07C49/67
摘要： The present invention provides substituted 3,3-diphenyl indole compounds, as well as analogues thereof, which are specific potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.
摘要翻译：本发明提供取代的3,3-二苯基吲哚化合物及其类似物，其是哺乳动物细胞增殖的特异性有效和安全的抑制剂。该化合物可用于抑制原位的哺乳动物细胞增殖，作为治疗或预防以异常细胞增殖为特征的疾病如癌症的治疗方法。

4. 发明授权

US07531573B2 Use of triaryl methane compounds for inhibiting unwanted cellular proliferation associated with inflammatory disease 有权
公开(公告)号：US07531573B2
公开(公告)日：2009-05-12
申请号：US10454372
申请日：2003-06-03
申请人： Carlo Brugnara , Jose Halperin , Emile M. Bellot, Jr. , Mark Froimowitz , Richard John Lombardy , John J. Clifford , Ying-Duo Gao , Reem M. Haidar , Eugene W. Kelleher , Falguni M. Kher , Adel M. Moussa , Yesh P. Sachdeva , Minghua Sun , Heather N. Taft
发明人： Carlo Brugnara , Jose Halperin , Emile M. Bellot, Jr. , Mark Froimowitz , Richard John Lombardy , John J. Clifford , Ying-Duo Gao , Reem M. Haidar , Eugene W. Kelleher , Falguni M. Kher , Adel M. Moussa , Yesh P. Sachdeva , Minghua Sun , Heather N. Taft
IPC分类号： A61K31/275
CPC分类号： A61K31/03 , A61K31/05 , A61K31/075 , A61K31/085 , A61K31/10 , A61K31/15 , A61K31/381 , C07C15/16 , C07C22/04 , C07C25/18 , C07C39/12 , C07C39/15 , C07C39/367 , C07C43/164 , C07C43/225 , C07C43/23 , C07C45/004 , C07C45/41 , C07C45/44 , C07C47/23 , C07C47/24 , C07C47/273 , C07C49/215 , C07C49/233 , C07C211/27 , C07C211/52 , C07C211/54 , C07C215/68 , C07C233/11 , C07C239/22 , C07C255/33 , C07C255/35 , C07C259/06 , C07C2601/14 , C07D207/26 , C07D213/16 , C07D213/20 , C07D213/30 , C07D295/145 , C07D307/33 , C07F7/0805 , C07F7/081 , C07F7/30 , C07F9/5352
摘要： The present invention provides a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation, and in particular inflammatory diseases associated with unwanted cellular proliferation. The active compounds are substituted triaryl methane compounds or analogues thereof where one or more of the aryl groups is replaced with a heteroaryl, cycloalkyl or heterocycloalkyl group and/or the tertiary carbon atom is replaced with a different atom such as Si, Ge, N or P. the compounds inhibit mammalian cell proliferation, inhibit the Gardos channel of erythrocytes, reduce sickle erythrocyte dehydration and/or delay the occurrence of erythrocyte sickling or deformation.

5. 发明授权

US06800658B2 Substituted diphenyl indanone, indane and indole compounds and analogues thereof useful for the treatment of prevention of diseases characterized by abnormal cell proliferation 失效
标题翻译：取代的二苯基二茚酮，二氢化茚和吲哚化合物及其类似物可用于治疗以异常细胞增殖为特征的疾病的治疗
公开(公告)号：US06800658B2
公开(公告)日：2004-10-05
申请号：US10043640
申请日：2002-01-10
申请人： Carlo Brugnara , Jose Halperin , Rudolf Fluckiger , Emile M. Bellott, Jr. , Richard John Lombardy , John J. Clifford , Ying-Duo Gao , Reem M. Haidar , Eugene W. Kelleher , Adel M. Moussa , Yesh P. Sachdeva , Minghua Sun , Heather N. Taft
发明人： Carlo Brugnara , Jose Halperin , Rudolf Fluckiger , Emile M. Bellott, Jr. , Richard John Lombardy , John J. Clifford , Ying-Duo Gao , Reem M. Haidar , Eugene W. Kelleher , Adel M. Moussa , Yesh P. Sachdeva , Minghua Sun , Heather N. Taft
IPC分类号： C07C2200
CPC分类号： C07D317/20 , C07C35/32 , C07C43/188 , C07C43/192 , C07C45/46 , C07C45/68 , C07C235/34 , C07C235/78 , C07C251/44 , C07C255/36 , C07C255/40 , C07C2602/08 , C07D209/40 , C07D303/46 , C07C49/697 , C07C49/67
摘要： The present invention provides substituted 3,3-diphenyl indanone, indane and indole compounds, as well as analogues thereof, which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.
摘要翻译：本发明提供取代的3,3-二苯基二茚酮，二氢化茚和吲哚化合物及其类似物，其是哺乳动物细胞增殖的特异性，有效和安全的抑制剂。该化合物可用于抑制原位的哺乳动物细胞增殖，作为治疗或预防以异常细胞增殖为特征的疾病如癌症的治疗方法。

6. 发明授权

US06541631B1 Methods of separating FTC isomers and derivatives thereof 有权
标题翻译：分离FTC异构体及其衍生物的方法
公开(公告)号：US06541631B1
公开(公告)日：2003-04-01
申请号：US09579796
申请日：2000-05-26
申请人： Salah Zahr , David A. Swanson , Adel M. Moussa , Luning Han
发明人： Salah Zahr , David A. Swanson , Adel M. Moussa , Luning Han
IPC分类号： C07D41104
CPC分类号： C07D411/04 , B01D15/185 , B01D15/3833 , Y02P20/55
摘要： The present invention relates to a method of preparing enantiomers and diastereomers of a 2′,3′-dideoxy-5-fluoro-3′thiocytadine (FTC) or a derivative thereof as represented by the following structural formula: In Structural Formula I, R is H, a substituted or unsubstituted organic acid radical, a substituted or unsubstituted alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted heteroaryl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted heteroaralkyl group, a substituted or unsubstituted cycloalkyl group, a substituted or unsubstituted heterocycloalkyl group, a substituted or unsubstituted cycloalkylalkyl, a substituted or unsubstituted heterocycloalkylalkyl, a sugar or a protecting group.
摘要翻译：本发明涉及如下结构式所示的制备2'，3'-二脱氧-5-氟-3'-硫代胞嘧啶（FTC）或其衍生物的对映异构体和非对映体的方法：在结构式I中，R 是取代或未取代的有机酸基，取代或未取代的烷基，取代或未取代的芳基，取代或未取代的杂芳基，取代或未取代的芳烷基，取代或未取代的杂芳烷基，取代或未取代的取代或未取代的杂环烷基，取代或未取代的环烷基烷基，取代或未取代的杂环烷基烷基，糖或保护基。

7. 发明授权

US10251903B2 Process for making nucleoside phosphoramidate compounds 有权
公开(公告)号：US10251903B2
公开(公告)日：2019-04-09
申请号：US15519846
申请日：2015-10-20
申请人： MERCK SHARP & DOHME CORP. , IDENIX Pharmaceuticals LLC , Bryon L. Simmons , Kevin R. Campos , Artis Klapars , Alistair J. Stewart , Benjamin A. Mayes , Peter E. Maligres , Alan Hyde , Steven Mark Silverman , Yong-Li Zhong , Adel M. Moussa , Kenneth Baker , Kara Van Valkenburg
发明人： Bryon L. Simmons , Kevin R. Campos , Artis Klapars , Alistair J. Stewart , Benjamin A. Mayes , Peter E. Maligres , Alan Hyde , Steven Mark Silverman , Yong-Li Zhong , Adel M. Moussa , Kenneth Baker , Kara Van Valkenburg
IPC分类号： C07H19/10 , A61K31/7052 , C07H1/00 , C08K3/08
摘要： The present invention is directed to a process for making Nucleoside Phosphoramidate Compounds of formula (I): which are useful for the treatment and prophylaxis of HCV infection. The present invention is also directed to compounds that are useful as synthetic intermediates for making the compounds of formula (I).

8. 发明授权

US08470870B2 Solid forms of an anti-HIV phosphoindole compound 失效
标题翻译：抗HIV磷酸吲哚化合物的固体形式
公开(公告)号：US08470870B2
公开(公告)日：2013-06-25
申请号：US12934627
申请日：2009-03-27
申请人： Adel M. Moussa , Mike H. O'Neill , Xiaohong Sheng
发明人： Adel M. Moussa , Mike H. O'Neill , Xiaohong Sheng
IPC分类号： A61K31/404 , C07D209/30
CPC分类号： C07F9/5728
摘要： Solid forms comprising a compound useful in the treatment, prevention and management of various conditions and diseases are provided herein. In particular, provided herein are solid forms comprising (2-carbamoyl-5-chloro-1H-indol-3-yl)-[3-((E)-2-cyano-vinyl)-5-methyl-phenyl]-(R)-phosphinic acid methyl ester, including salts thereof, having utility for the treatment, prevention and management of conditions and disorders including, but not limited to, human immunodeficiency virus infection.
摘要翻译：本文提供了包含可用于治疗，预防和治疗各种病症和疾病的化合物的固体形式。特别地，本文提供了包含（2-氨基甲酰基-5-氯-1H-吲哚-3-基） - [3 - （（E）-2-氰基 - 乙烯基）-5-甲基 - 苯基] - （ R） - 次膦酸甲酯，包括其盐，可用于治疗，预防和治疗病症和病症，包括但不限于人类免疫缺陷病毒感染。

9. 发明申请

US20110039803A1 SOLID FORMS OF AN ANTI-HIV PHOSPHOINDOLE COMPOUND 失效
标题翻译：抗HIV磷酸二酯化合物的固体形式
公开(公告)号：US20110039803A1
公开(公告)日：2011-02-17
申请号：US12934627
申请日：2009-03-27
申请人： Adel M. Moussa , Mike H. O'Neill , Xiaohong Sheng
发明人： Adel M. Moussa , Mike H. O'Neill , Xiaohong Sheng
IPC分类号： A61K31/675 , C07F9/30 , A61P31/18
CPC分类号： C07F9/5728
摘要： Solid forms comprising a compound useful in the treatment, prevention and management of various conditions and diseases are provided herein. In particular, provided herein are solid forms comprising (2-carbamoyl-5-chloro-1H-indol-3-yl)-[3-((E)-2-cyano-vinyl)-5-methyl-phenyl]-(R)-phosphinic acid methyl ester, including salts thereof, having utility for the treatment, prevention and management of conditions and disorders including, but not limited to, human immunodeficiency virus infection.
摘要翻译：本文提供了包含可用于治疗，预防和治疗各种病症和疾病的化合物的固体形式。特别地，本文提供了包含（2-氨基甲酰基-5-氯-1H-吲哚-3-基） - [3 - （（E）-2-氰基 - 乙烯基）-5-甲基 - 苯基] - （ R） - 次膦酸甲酯，包括其盐，可用于治疗，预防和治疗病症和病症，包括但不限于人类免疫缺陷病毒感染。

10. 发明授权

US06992079B2 Substituted 11-phenyl-dibenzazepine compounds useful for the treatment or prevention of diseases characterized by abnormal cell proliferation 失效
公开(公告)号：US06992079B2
公开(公告)日：2006-01-31
申请号：US10013308
申请日：2001-12-07
申请人： Carlo Brugnara , Jose Halperin , Rudolf Fluckiger , Emile M. Bellott, Jr. , Richard John Lombardy , John J. Clifford , Ying-Duo Gao , Reem M. Haidar , Eugene W. Kelleher , Adel M. Moussa , Yesh P. Sachdeva , Minghua Sun , Heather N. Taft , Michael H. Zeldin
发明人： Carlo Brugnara , Jose Halperin , Rudolf Fluckiger , Emile M. Bellott, Jr. , Richard John Lombardy , John J. Clifford , Ying-Duo Gao , Reem M. Haidar , Eugene W. Kelleher , Adel M. Moussa , Yesh P. Sachdeva , Minghua Sun , Heather N. Taft , Michael H. Zeldin
IPC分类号： A61K31/55 , C07D233/18
CPC分类号： C07D223/20
摘要： The present invention provides substituted 11-phenyl-dibenzazepine compounds which are specific, potent and safe inhibitors of mammalian cell proliferation. The compounds can be used to inhibit mammalian cell proliferation in situ as a therapeutic approach towards the treatment or prevention of diseases characterized by abnormal cell proliferation, such as cancer.

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