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1. 发明申请

US20050227965A1 Crystalline polymorph of bazedoxifene acetate 有权
标题翻译：巴多昔芬乙酸酯的结晶多晶型物
公开(公告)号：US20050227965A1
公开(公告)日：2005-10-13
申请号：US11100983
申请日：2005-04-06
申请人： Christopher Demerson , Silvio Iera , Kadum Ali
发明人： Christopher Demerson , Silvio Iera , Kadum Ali
IPC分类号： A61K31/55 , C07D209/12 , C07D403/12 , C07D43/02
CPC分类号： C07D209/12 , C07D403/12
摘要： The present invention is directed to a crystalline polymorph of bazedoxifene acetate, compositions containing the same, preparations thereof, and uses thereof.
摘要翻译：本发明涉及乙酸巴多昔芬的结晶多晶型物，含有它们的组合物，其制备方法及其应用。

2. 发明授权

US07683051B2 Crystalline polymorph of bazedoxifene acetate 有权
公开(公告)号：US07683051B2
公开(公告)日：2010-03-23
申请号：US11100983
申请日：2005-04-06
申请人： Christopher Demerson , Silvio Iera , Kadum A. Ali
发明人： Christopher Demerson , Silvio Iera , Kadum A. Ali
IPC分类号： A61P5/30 , A61K31/55 , C07D403/02
CPC分类号： C07D209/12 , C07D403/12
摘要： The present invention is directed to a crystalline polymorph of bazedoxifene acetate, compositions containing the same, preparations thereof, and uses thereof.

3. 发明申请

US20050038026A1 Preparation and purification of antiviral disulfonic acid disodium salt 失效
标题翻译：抗病毒二磺酸二钠盐的制备与纯化
公开(公告)号：US20050038026A1
公开(公告)日：2005-02-17
申请号：US10946842
申请日：2004-09-22
申请人： Silvio Iera , Christopher Demerson , Jacqueline Lunetta , Maria Papamichelakis , Michael MacEwan , Wayne McMahon , John Potoski , Arthur Mohan
发明人： Silvio Iera , Christopher Demerson , Jacqueline Lunetta , Maria Papamichelakis , Michael MacEwan , Wayne McMahon , John Potoski , Arthur Mohan
IPC分类号： C07C303/38 , C07C303/40 , C07C311/19 , C07C311/42 , C07D251/50 , C07D251/70 , C07D251/48 , A61K31/53
CPC分类号： C07C303/38 , C07C303/40 , C07D251/50 , C07D251/70 , C07C311/19 , C07C311/42
摘要： The present invention provides a new process and intermediates for the production of antiviral compound 4′,4-bis-{4,6-bis-[3-(bis-carbamoyl-methyl-1-sulfamoyl)-phenylamino]-[1,3,5]triazin-2-ylamino}-biphenyl-2,2′-disulfonic acid and its pharmaceutically acceptable salts.
摘要翻译：本发明提供了用于制备抗病毒化合物4'，4-双 - {4,6-双 - [3-（双 - 氨基甲酰基 - 甲基-1-氨磺酰基） - 苯基氨基] - [ 3,5]三嗪-2-基氨基} - 联苯-2,2'-二磺酸及其药学上可接受的盐。

4. 发明申请

US20060199967A1 Process for the purification of substituted benzoxazole compounds 失效
公开(公告)号：US20060199967A1
公开(公告)日：2006-09-07
申请号：US11369113
申请日：2006-03-06
申请人： Silvio Iera
发明人： Silvio Iera
IPC分类号： C07D263/60
CPC分类号： C07D263/57 , C07D263/42
摘要： The present invention provides processes for the purification of substituted benzoxazole compounds, and in particular 2-(3-fluoro-4-hydroxy-phenyl)-7-vinyl-benzooxazol-5-ol. The processes include recrystallizing the compound from a solution comprising acetone and acetonitrile; treating the crude purified product with a clarifying agent in a solution comprising ethyl acetate, and precipitating or triturating the compound from a mixed solvent system.

5. 发明授权

US06693197B2 Process for the synthesis of derivatives of 2,3-dihydro-1,4-dioxino- [2,3-f] quinoline 失效
标题翻译：合成2,3-二氢-1,4-二氧杂 - [2,3-f]喹啉衍生物的方法
公开(公告)号：US06693197B2
公开(公告)日：2004-02-17
申请号：US10145369
申请日：2002-05-14
申请人： Anita W. Chan , Timothy T. Curran , Silvio Iera , Warren Chew , John H. Sellstedt , Galina Vid , Gregg Feigelson , Zhixian Ding
发明人： Anita W. Chan , Timothy T. Curran , Silvio Iera , Warren Chew , John H. Sellstedt , Galina Vid , Gregg Feigelson , Zhixian Ding
IPC分类号： C07D49102
CPC分类号： C07D491/04
摘要： Methods of preparing compounds of Formula I are provided.
摘要翻译：提供制备式Iare化合物的方法。

6. 发明授权

US06268504B1 Aryloxy-alkyl-dialkylamines 失效
标题翻译：芳氧基 - 烷基 - 二烷基胺
公开(公告)号：US06268504B1
公开(公告)日：2001-07-31
申请号：US09458317
申请日：1999-12-10
申请人： Panolil Raveendranath , Joseph Zeldis , Galina Vid , John R. Potoski , Jianxin Ren , Silvio Iera
发明人： Panolil Raveendranath , Joseph Zeldis , Galina Vid , John R. Potoski , Jianxin Ren , Silvio Iera
IPC分类号： C07D27704
CPC分类号： C07D295/088 , C07C217/48
摘要： The present invention provides compounds useful in the synthesis of biologically active compounds, and processes for their production, the compounds having the formula: wherein: R1 and R2 are, independently, selected from H; C1-C12 alkyl or C1-C6 perfluorinated alkyl; X represents a leaving group; A is O or S; m is an integer from 1 to 3, preferably 2; R3, R4, R5, and R6 are independently selected from H, halogen, —NO2, alkyl, alkoxy, C1-C6 perfluorinated alkyl, OH or the C1-C4 esters or alkyl ethers thereof, —CN, —O—R1, —O—Ar, —S—R1, —S—Ar, —SO—R1, —SO—Ar, —SO2—R1, —SO2—Ar, —CO—R1, —CO—Ar, —CO2—R1, or —CO2—Ar; and Y is selected from a) the moiety: wherein R7 and R8 are independently selected from the group of H, C1-C6 alkyl, or phenyl; or b) an optionally substituted five-, six- or seven-membered saturated, unsaturated or partially unsaturated heterocycle or bicyclic heterocycle containing up to two heteroatoms selected from the group consisting of —O—, —NH—, —N(C1C4 alkyl)—, —N═, and —S(O)n—.
摘要翻译：本发明提供了可用于合成生物活性化合物的化合物及其制备方法，具有下式的化合物：其中：R 1和R 2独立地选自H; C1-C12烷基或C1-C6全氟化烷基; X表示离去基团; A是O或S; m为1〜3的整数，优选为2; R 3，R 4，R 5和R 6独立地选自H，卤素，-NO 2，烷基，烷氧基，C 1 -C 6全氟烷基，OH或其C 1 -C 4酯或其烷基醚，-CN，-O-R 1， O-Ar，-S-R 1，-S-Ar，-SO-R 1，-SO-Ar，-SO 2 -R 1，-SO 2 -Ar，-CO-R 1，-CO-Ar，-CO 2 -R -CO 2 -Ar; 并且Y选自a）部分：其中R 7和R 8独立地选自H，C 1 -C 6烷基或苯基; 或b）任选取代的五元，六元或七元饱和的不饱和或部分不饱和的杂环或双环杂环，其含有至多两个选自-O - ， - NH - ， - N（C 1 -C 4烷基） - ， - N =和-S（O）n - 。

7. 发明授权

US5760220A Process for preparation of biphenyl derivatives 失效
标题翻译：联苯衍生物的制备方法
公开(公告)号：US5760220A
公开(公告)日：1998-06-02
申请号：US657490
申请日：1996-06-04
申请人： Pierre Giguere , Silvio Iera , Michel Bernatchez , Giuseppe Barreca , Graziano Castaldi , Vincenzo Cannata
发明人： Pierre Giguere , Silvio Iera , Michel Bernatchez , Giuseppe Barreca , Graziano Castaldi , Vincenzo Cannata
IPC分类号： C07D471/04 , C07D257/04 , C07D487/04
CPC分类号： C07D471/04 , Y02P20/55
摘要： A process is described for preparing a compound of the formula I: ##STR1## or a salt thereof; wherein X is a protecting group and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently hydrogen, C.sub.1-6 alkyl or C.sub.1-6 perfluoroalkyl, R.sub.5 is hydrogen or when n is 1 R.sub.5 taken together with R.sub.3 comprises a double bond; m is 1, 2 or 3; n is 0 or 1, and p is 0, 1 or 2.
摘要翻译：描述了制备式I化合物或其盐的方法：其中X是保护基，R 1，R 2，R 3和R 4各自独立地是氢，C 1-6烷基或C 1-6全氟烷基，R 5是氢或当n是1时，R 5与R 3一起包括双键; m为1,2或3; n为0或1，p为0,1或2。

8. 发明授权

US07683182B2 Crystal forms of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol 失效
标题翻译： 2-（3-氟-4-羟基苯基）-7-乙烯基-1,3-苯并恶唑-5-醇的晶型
公开(公告)号：US07683182B2
公开(公告)日：2010-03-23
申请号：US11369405
申请日：2006-03-06
申请人： Abdolsamad Tadayon , Silvio Iera , Hong Wen , Marc S. Tesconi , Mannching Sherry Ku
发明人： Abdolsamad Tadayon , Silvio Iera , Hong Wen , Marc S. Tesconi , Mannching Sherry Ku
IPC分类号： C07D263/58
CPC分类号： C07D263/57
摘要： The present invention is directed to monohydrate and anhydrate crystal forms of 2-(3-fluoro-4-hydroxyphenyl)-7-vinyl-1,3-benzoxazol-5-ol, an estrogenic receptor modulator useful in the treatment of, for example, diseases related to abnormal levels of estrogen.
摘要翻译：本发明涉及2-（3-氟-4-羟基苯基）-7-乙烯基-1,3-苯并恶唑-5-醇的一水合物和无水晶体形式，可用于例如治疗的雌激素受体调节剂，与异常水平的雌激素相关的疾病。

9. 再颁专利

USRE41084E1 Antineoplastic combinations 失效
标题翻译：抗肿瘤药物组合
公开(公告)号：USRE41084E1
公开(公告)日：2010-01-19
申请号：US11645327
申请日：2006-12-22
申请人： John Leo Considine , Sylvain Daigneault , Warren Chew , Silvio Iera , Scott Duncan , Jiaxen Ren
发明人： John Leo Considine , Sylvain Daigneault , Warren Chew , Silvio Iera , Scott Duncan , Jiaxen Ren
IPC分类号： A61K31/44
CPC分类号： A61K31/00 , A61K31/395 , A61K31/436 , A61K31/47 , A61K31/4706 , C07C229/30 , C07C237/16 , Y10S514/922 , A61K2300/00
摘要： This invention provides the use of a combination of CCI-779 and EKB-569 in the treatment of neoplasms.
摘要翻译：本发明提供CCI-779和EKB-569的组合在肿瘤治疗中的用途。

10. 发明授权

US07038052B2 Process for the synthesis of derivatives of 2, 3-dihydro-1, 4-dioxino- [2, 3-f] quinoline 失效
标题翻译：合成2,3-二氢-1,4-二氧杂环己烯并[2,3-f]喹啉衍生物的方法
公开(公告)号：US07038052B2
公开(公告)日：2006-05-02
申请号：US10734867
申请日：2003-12-12
申请人： Anita W. Chan , Timothy T. Curran , Silvio Iera , Warren Chew , John H. Sellstedt , Galina Vid , Gregg Feigelson , Zhixian Ding
发明人： Anita W. Chan , Timothy T. Curran , Silvio Iera , Warren Chew , John H. Sellstedt , Galina Vid , Gregg Feigelson , Zhixian Ding
IPC分类号： C07D491/02 , C07D491/06
CPC分类号： C07D491/04
摘要： Methods of preparing compounds of Formula I are provided.
摘要翻译：提供制备式I化合物的方法。

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