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1. 发明申请

US20080177029A1 Process for preparing macrocyclic compounds 有权
标题翻译：制备大环化合物的方法
公开(公告)号：US20080177029A1
公开(公告)日：2008-07-24
申请号：US11670140
申请日：2007-02-01
申请人： Carl Alan Busacca , Vittorio Farina , Fabrice Gallou , Nizar Haddad , Xiao-Jun Wang , Xudong Wei , Jinghua Xu , Yibo Xu , Nathan K. Yee , Li Zhang
发明人： Carl Alan Busacca , Vittorio Farina , Fabrice Gallou , Nizar Haddad , Xiao-Jun Wang , Xudong Wei , Jinghua Xu , Yibo Xu , Nathan K. Yee , Li Zhang
IPC分类号： C07K5/12 , C07D215/00
CPC分类号： C07K5/0802 , A61K38/00 , C07D417/14 , C07K1/006 , C07K5/06165 , C07K5/0827
摘要： Disclosed is a multi-step process for preparing a macrocyclic compound of the formula (I): wherein Q is a radical of the following formula: and the other variables are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.
摘要翻译：公开了用于制备式（I）的大环化合物的多步骤方法：其中Q是下式的基团：其它变量如本文所定义。式（I）化合物是用于治疗丙型肝炎病毒（HCV）感染的有效活性剂。

2. 发明授权

US5693666A 6,7-modified paclitaxels 失效
标题翻译： 6,7修饰紫杉醇
公开(公告)号：US5693666A
公开(公告)日：1997-12-02
申请号：US582322
申请日：1996-01-03
申请人： Shu-Hui Chen , Vittorio Farina , Gregory Roth , John Kadow
发明人： Shu-Hui Chen , Vittorio Farina , Gregory Roth , John Kadow
IPC分类号： A61K31/337 , A61P35/00 , C07D305/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07F7/18 , A61K31/335
CPC分类号： C07D407/12 , C07D305/14 , C07D409/12 , C07D413/12 , C07F7/1856
摘要： The present invention provides paclitaxel derivatives of formula I ##STR1## and pharmaceutical compositions.
摘要翻译：本发明提供式I的紫杉醇衍生物和药物组合物。

3. 发明授权

US5380751A 6,7-modified paclitaxels 失效
标题翻译： 6,7修饰紫杉醇
公开(公告)号：US5380751A
公开(公告)日：1995-01-10
申请号：US128619
申请日：1993-09-28
申请人： Shu-Hui Chen , Vittorio Farina , Gregory Roth , John Kadow
发明人： Shu-Hui Chen , Vittorio Farina , Gregory Roth , John Kadow
IPC分类号： A61K31/337 , A61P35/00 , C07D305/14 , C07D407/12 , C07D409/12 , C07D413/12 , C07F7/18 , A61K31/335
CPC分类号： C07D407/12 , C07D305/14 , C07D409/12 , C07D413/12 , C07F7/1856
摘要： The present invention provides paclitaxel derivatives of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.Z is RO-- or R;R.sup.2 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, phenyl, or heteroaryl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.a is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR;R.sup.b and R.sup.c are both hydroxy or together form a bond with the carbon atoms to which they are attached; andR and R.sup.o are independently C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.3-6 cycloalkyl, C.sub.2-6 alkynyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups.Also provided by this invention are pharmaceutical formulations (compositions) and a method of treating mammalian tumors with a compound of formula I.
摘要翻译：本发明提供式I的紫杉醇衍生物，其中R 1是其中R Z是RO-或R的-CORz; R 2是C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基或式-W-Rx的基团，其中W是键，C 2-6亚烯基或 - （CH 2）t - 其中t为1至6; 并且Rx是萘基，苯基或杂芳基，此外Rx可任选地被一至三个相同或不同的C 1-6烷基，C 1-6烷氧基，卤素或-CF 3基团取代; R a是-OCOR，H，OH，-OR，-OSO 2 R，-OCONRoR，-OCONHR，-OCOO（CH 2）t R或-OCOOR; Rb和Rc都是羟基或与它们所连接的碳原子一起形成键; 并且R和R 4独立地是C 1-6烷基，C 2-6烯基，C 3-6环烷基，C 2-6炔基或苯基，任选地被一至三个相同或不同的C 1-6烷基，C 1-6烷氧基，卤素或 -CF3组。本发明还提供了药物制剂（组合物）和用式I化合物治疗哺乳动物肿瘤的方法。

4. 发明授权

US5162521A Processes for making cephems from allenylazetidinone derivatives 失效
标题翻译：从烯丙基氮杂环丁酮衍生物制备头孢烯的方法
公开(公告)号：US5162521A
公开(公告)日：1992-11-10
申请号：US711250
申请日：1991-06-06
申请人： Vittorio Farina , Stephen R. Baker
发明人： Vittorio Farina , Stephen R. Baker
IPC分类号： C07D501/00 , C07D501/10
CPC分类号： C07D501/00 , Y02P20/55
摘要： This invention relates to a novel process for making a cephem of formula II from 2-(3-amino-2-oxo-azetidin-1-yl)-2,3-butadienoate of formula I. In another aspect, this invention is concerned with a process of further converting a compound of formula II into an antibacterial cephem of formula III. ##STR1## In formulae I, II and III, R.sup.1 is hydrogen, a conventional amino protecting group or an acyl group; R.sup.2 is an aromatic heterocyclic or aryl group; R.sup.3 is a conventional carboxy protecting group or --CO.sub.2 R.sup.3 taken together forms a physiologically hydrolyzable ester; and R.sup.4 is a group selected from the group consisting of C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, cyclic C.sub.3-6 alkyl, and aryl; and n is 0 or 2.
摘要翻译：本发明涉及由式I的2-（3-氨基-2-氧代 - 氮杂环丁烷-1-基）-2,3-丁二烯酸制备式II的头孢烯的新方法。另一方面，本发明涉及其具有将式II化合物进一步转化成式III的抗菌头孢烯的方法。在式I，II和III中，R 1是氢，常规的氨基保护基或酰基; R2是芳族杂环或芳基; R3是常规的羧基保护基或-CO 2 R 3一起形成生理上可水解的酯; 并且R 4是选自C 1-6烷基，C 2-6烯基，C 2-6炔基，环C 3-6烷基和芳基的基团。 n为0或2。

5. 发明授权

US06407238B1 Process of making substituted pyrazoles 有权
标题翻译：制备取代的吡唑的方法
公开(公告)号：US06407238B1
公开(公告)日：2002-06-18
申请号：US09698442
申请日：2000-10-27
申请人： James A. Baron , Vittorio Farina , Nizar Haddad
发明人： James A. Baron , Vittorio Farina , Nizar Haddad
IPC分类号： C07D40304
CPC分类号： C07D231/12
摘要： Disclosed is a process of making substituted pyrazoles from substituted benzophenone hydrazones with a variety of 1,3-bifunctional substrates under acid conditions. The pyrazole compounds are useful for making pharmaceutical compounds.
摘要翻译：公开了在酸性条件下由具有各种1,3-双官能底物的取代的二苯甲酮腙制备取代的吡唑的方法。吡唑化合物可用于制备药物化合物。

6. 发明授权

US5254580A 7,8-cyclopropataxanes 失效
标题翻译： 7,8-环丙烷
公开(公告)号：US5254580A
公开(公告)日：1993-10-19
申请号：US29819
申请日：1993-03-11
申请人： Shu-Hui Chen , Vittorio Farina
发明人： Shu-Hui Chen , Vittorio Farina
IPC分类号： C07D305/14 , A01N43/02 , C07C305/00
CPC分类号： C07D305/14
摘要： An antitumor compound of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.z is t-butyloxy, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or phenyl, optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.2 is C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.3-6 cycloalkyl, or a radical of the formula --W--R.sup.x in which W is a bond, C.sub.2-6 alkenediyl, or --(CH.sub.2).sub.t --, in which t is one to six; and R.sup.x is naphthyl, furyl, thienyl or phenyl, and furthermore R.sup.x can be optionally substituted with one to three same or different C.sub.1-6 alkyl, C.sub.1-6 alkoxy, halogen or --CF.sub.3 groups;R.sup.3 is OCOR, --OCOOR, H, or OH; R.sup.4 is hydrogen; or R.sup.3 and R.sup.4 jointly form a carbonyl group; and R is C.sub.1-6 alkyl.Also provided by this invention are pharmaceutical formulations (compositions) and a method of treating mammalian tumors with a compound of formula I.
摘要翻译：式I的抗肿瘤化合物，其中R 1为-COR z，其中R z为叔丁氧基，C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基或苯基，任选被一至三个相同或不同的C 1-6烷基，C 1-6烷氧基，卤素或-CF 3基团; R 2是C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基或式-W-Rx的基团，其中W是键，C 2-6亚烯基或 - （CH 2）t - 其中t为1至6; 并且Rx是萘基，呋喃基，噻吩基或苯基，此外Rx可以任选地被一至三个相同或不同的C 1-6烷基，C 1-6烷氧基，卤素或-CF 3基团取代; R3是OCOR，-OCOOR，H或OH; R4是氢; 或R3和R4共同形成羰基; 且R为C 1-6烷基。本发明还提供了药物制剂（组合物）和用式I化合物治疗哺乳动物肿瘤的方法。

7. 发明申请

US20110087017A1 PROCESS FOR THE PREPARATION OF COMPOUNDS USEFUL AS INHIBITORS OF SGLT2 有权
标题翻译：制备作为SGLT2的抑制剂的化合物的方法
公开(公告)号：US20110087017A1
公开(公告)日：2011-04-14
申请号：US12904233
申请日：2010-10-14
申请人： Vittorio FARINA , Sebastien François Emmanuel Lemaire , Ioannis N. Houpis
发明人： Vittorio FARINA , Sebastien François Emmanuel Lemaire , Ioannis N. Houpis
IPC分类号： C07H1/00 , C07H13/04 , C07H7/06 , C07F3/06
CPC分类号： C07D409/14 , C07D309/10 , C07D409/10 , C07F3/06 , Y02P20/55
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。

8. 发明授权

US07714127B2 Process for making heteroaryl amine intermediate compounds 有权
标题翻译：制备杂芳基胺中间体化合物的方法
公开(公告)号：US07714127B2
公开(公告)日：2010-05-11
申请号：US11538465
申请日：2006-10-04
申请人： Guisheng Li , Jianxiu Liu , Zhi-Hui (Bruce) Lu , Ming Shen , Sonia Rodriguez , Vittorio Farina
发明人： Guisheng Li , Jianxiu Liu , Zhi-Hui (Bruce) Lu , Ming Shen , Sonia Rodriguez , Vittorio Farina
IPC分类号： C07D413/06
CPC分类号： C07D213/38
摘要： Disclosed are processes to produce a compound of the formula (I):
摘要翻译：公开了制备式（I）化合物的方法：

9. 发明申请

US20070105857A1 Process for Making Heteroaryl Amine Intermediate Compounds 有权
标题翻译：制备杂芳基中间体化合物的方法
公开(公告)号：US20070105857A1
公开(公告)日：2007-05-10
申请号：US11538465
申请日：2006-10-04
申请人： Guisheng Li , Jianxiu Liu , Zhi-Hui (Bruce) Lu , Ming Shen , Sonia Rodriguez , Vittorio Farina
发明人： Guisheng Li , Jianxiu Liu , Zhi-Hui (Bruce) Lu , Ming Shen , Sonia Rodriguez , Vittorio Farina
IPC分类号： A61K31/5377 , C07D413/02
CPC分类号： C07D213/38
摘要： Disclosed are processes to produce a compound of the formula (I):
摘要翻译：公开了制备式（I）化合物的方法：

10. 发明申请

US20050209135A1 Process for preparing macrocyclic compounds 审中-公开
标题翻译：制备大环化合物的方法
公开(公告)号：US20050209135A1
公开(公告)日：2005-09-22
申请号：US11078074
申请日：2005-03-11
申请人： Carl Busacca , Vittorio Farina , Fabrice Gallou , Nizar Haddad , Xiao-Jun Wang , Xudong Wei , Jinghua Xu , Yibo Xu , Nathan Yee , Li Zhang
发明人： Carl Busacca , Vittorio Farina , Fabrice Gallou , Nizar Haddad , Xiao-Jun Wang , Xudong Wei , Jinghua Xu , Yibo Xu , Nathan Yee , Li Zhang
IPC分类号： A61K31/4709 , A61K38/00 , A61K38/12 , C07D417/14 , C07K1/00 , C07K5/06 , C07K5/078 , C07K5/08 , C07K5/12
CPC分类号： C07K5/0802 , A61K38/00 , C07D417/14 , C07K1/006 , C07K5/06165 , C07K5/0827
摘要： Disclosed is a multi-step process for preparing a macrocyclic compound of the formula (I): wherein Q is a radical of the following formula: and the other variables are as defined herein. The compounds of formula (I) are potent active agents for the treatment of hepatitis C virus (HCV) infection.
摘要翻译：公开了用于制备式（I）的大环化合物的多步方法：其中Q是下式的基团：其它变量如本文所定义。式（I）化合物是用于治疗丙型肝炎病毒（HCV）感染的有效活性剂。

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