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1. 发明申请

US20100145099A1 NOVEL POLYMORPHIC FORMS OF MILNACIPRAN HYDROCHLORIDE 审中-公开
标题翻译： MILNACIPRAN HYDROCHLORIDE的新型多晶型
公开(公告)号：US20100145099A1
公开(公告)日：2010-06-10
申请号：US12528983
申请日：2008-02-28
申请人： Roshan Ramesh Medhane , Nitin Maheswari , Keshav Deo , Mohan Prasad , Joydeep Kant
发明人： Roshan Ramesh Medhane , Nitin Maheswari , Keshav Deo , Mohan Prasad , Joydeep Kant
IPC分类号： C07C237/00
CPC分类号： C07C237/24 , C07B2200/07 , C07B2200/13 , C07C2601/02
摘要： The present invention relates to polymorphic forms of milnacipran hydrochloride. The polymorphic forms are designated as Form (I), Form (II), Form (III), Form (IV) and Form V of milnacipran hydrochloride. The present invention also relates to processes for the preparation of the polymorphic forms.
摘要翻译：本发明涉及盐酸米那普仑的多晶型物质。多晶型物被命名为盐酸米那普仑的形式（I），形式（II），形式（III），形式（IV）和形式V. 本发明还涉及制备多晶型物的方法。

2. 发明申请

US20090326263A1 Process for the preparation of aniline-derived thyroid receptor ligands 失效
标题翻译：制备苯胺衍生甲状腺受体配体的方法
公开(公告)号：US20090326263A1
公开(公告)日：2009-12-31
申请号：US12456313
申请日：2009-06-15
申请人： Ramakrishnan Chidambaram , Joydeep Kant , Raymond E. Weaver , Jurong Yu , Arun Ghosh
发明人： Ramakrishnan Chidambaram , Joydeep Kant , Raymond E. Weaver , Jurong Yu , Arun Ghosh
IPC分类号： C07C309/24 , C07C205/12 , C07C37/04 , C07C47/56
CPC分类号： C07C309/65 , C07C45/00 , C07C201/12 , C07C205/12 , C07C205/37 , C07C205/38 , C07C205/43 , C07C213/02 , C07C231/02 , C07C233/25 , C07C309/24 , C07C47/575 , C07C217/90
摘要： Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.
摘要翻译：提供了合成苯胺衍生物的方法，特别是具有作为甲状腺受体配体活性的某些苯胺衍生物。

3. 发明申请

US20050054863A1 Process for preparing 4-alkyl- or 4-aryl-oxycarbonyl paclitaxel analogs and novel intermediates 失效
标题翻译：制备4-烷基 - 或4-芳基 - 氧羰基紫杉醇类似物和新型中间体的方法
公开(公告)号：US20050054863A1
公开(公告)日：2005-03-10
申请号：US10909899
申请日：2004-08-02
申请人： Frank Gibson , Joydeep Kant , Rajendra Deshpande , Karen TenHuisen , Jing Liang , Jun Li , Susan Boettger , Edward Gublo , Ulhas Dhokte
发明人： Frank Gibson , Joydeep Kant , Rajendra Deshpande , Karen TenHuisen , Jing Liang , Jun Li , Susan Boettger , Edward Gublo , Ulhas Dhokte
IPC分类号： C07D305/14 , C07D35/14
CPC分类号： C07D305/14 , Y02P20/55
摘要： A process is provided for preparing 4-alkyl- or 4-aryl-oxycarbonyl paclitaxel analogs which includes the steps of converting paclitaxel into a C-7 acylprotected paclitaxel employing an electrophilic protecting group, such as benzoyloxycarbonyl, and converting the C-7 protected analog into the 4-alkyloxycarbonyl or 4-aryloxycarbonyl paclitaxel analog. Novel intermediates produced in the process are also provided.
摘要翻译：提供一种制备4-烷基 - 或4-芳基 - 氧羰基紫杉醇类似物的方法，其包括使用亲电保护基如苯甲酰氧基羰基将紫杉醇转化为C-7酰基保护的紫杉醇的步骤，并将C-7保护的类似物进入4-烷氧基羰基或4-芳氧基羰基紫杉醇类似物。还提供了在该方法中生产的新型中间体。

4. 发明授权

US5294637A Fluoro taxols 失效
标题翻译：氟紫杉醇
公开(公告)号：US5294637A
公开(公告)日：1994-03-15
申请号：US62687
申请日：1993-05-20
申请人： Shu-Hui Chen , Vittorio Farina , Joydeep Kant , Dolatrai M. Vyas
发明人： Shu-Hui Chen , Vittorio Farina , Joydeep Kant , Dolatrai M. Vyas
IPC分类号： C07D305/14 , C07D407/12 , C07D409/12 , C07F7/18 , C07F9/655 , C07F9/6558 , H01L21/48 , H05K1/03 , H05K1/09 , H05K1/16 , H05K3/40 , A01N43/02 , C07D305/00
CPC分类号： C07D407/12 , C07D305/14 , C07D409/12 , C07F7/1856 , C07F9/65512 , C07F9/65586 , H01L21/4839 , H05K1/16 , H05K1/0306 , H05K1/092 , H05K3/403
摘要： This invention relates to a fluorinated taxol of formula I ##STR1## in which R.sup.1 is --COR.sup.z in which R.sup.z is RO-- or R;R.sup.g 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.2 is --OCOR, H, OH, --OR, --OSO.sub.2 R, --OCONR.sup.o R, --OCONHR, --OCOO(CH.sub.2).sub.t R, or --OCOOR; 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.Further provided by this invention are pharmaceutical formulations and useful intermediates for the fluorinated taxols of formula I. A method of treating mammalian tumors using a compound of formula I is also provided.
摘要翻译：本发明涉及式I的氟化紫杉醇，其中R 1是-COR 3，其中R z是RO-或R; R 8为C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基或W-Rx基团，W为键，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; R2是-OCOR，H，OH，-OR，-OSO2R，-OCONRoR，-OCONHR，-OCOO（CH2）tR或-OCOOR; 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。本发明进一步提供了用于式I的氟化紫杉醇的药物制剂和有用的中间体。还提供了使用式I化合物治疗哺乳动物肿瘤的方法。

5. 发明授权

US5266691A 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：US5266691A
公开(公告)日：1993-11-30
申请号：US928863
申请日：1992-08-11
申请人： Vittorio Farino , Joydeep Kant
发明人： Vittorio Farino , Joydeep Kant
IPC分类号： C07D205/095 , C07D417/12 , C07D501/00 , C07D501/08 , C07D501/22 , C07D501/36 , A61K31/545
CPC分类号： C07D417/12 , C07D205/095 , C07D501/00 , Y02P20/55
摘要： This invention relates to a novel process for making a cephem of formula II from a 2-(3-amino-2-oxo-azetidin-1-yl)-2,3-butadienoate intermediate of formula I using an organo-copper reagent. In another aspect, this invention is concerned with said intermediate. ##STR1## In the compounds of Scheme (A), R.sup.1 is 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：本发明涉及使用有机铜试剂从式（I）的2-（3-氨基-2-氧代 - 氮杂环丁烷-1-基）-2,3-丁二烯酸中间体制备式II头孢的新方法。另一方面，本发明涉及所述中间体。（A）在方案（A）的化合物中，R 1是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。

6. 发明授权

US5043439A Process for production of cephalosporins 失效
标题翻译：生产头孢菌素的方法
公开(公告)号：US5043439A
公开(公告)日：1991-08-27
申请号：US490213
申请日：1990-03-08
申请人： Joydeep Kant , Chester Sapino, Jr.
发明人： Joydeep Kant , Chester Sapino, Jr.
IPC分类号： C07D501/02 , C07D501/00 , C07D501/04 , C07D501/10
CPC分类号： C07D501/00
摘要： Cephalosporin intermediates having a replacable organosulfonylyoxy or heterocyclothio group in the 3-position undergo a carbon alkylation process with organocopper reagents to provide 3-hydrocarbon substituted cephalosporin antibiotics.
摘要翻译：在3位上具有可替换的有机磺酰氧基或杂环硫基的头孢菌素中间体通过有机铜试剂进行碳烷基化方法以提供3-烃取代的头孢菌素抗生素。

7. 发明授权

US06875867B2 Process for preparing chiral diol sulfones and dihydroxy acid HMG CoA reductase inhibitors 失效
标题翻译：制备手性二醇砜和二羟基酸HMG CoA还原酶抑制剂的方法
公开(公告)号：US06875867B2
公开(公告)日：2005-04-05
申请号：US10158355
申请日：2002-05-30
申请人： Paul R. Brodfuehrer , Thomas R. Sattelberg , Joydeep Kant , Xinhua Qian
发明人： Paul R. Brodfuehrer , Thomas R. Sattelberg , Joydeep Kant , Xinhua Qian
IPC分类号： C07D239/26 , A61K31/435 , A61K31/4353 , A61P3/06 , A61P43/00 , C07B53/00 , C07C67/283 , C07C69/30 , C07D207/34 , C07D213/55 , C07D221/16 , C07D309/30 , C07D319/06 , C07D405/06 , C07D405/12 , C07D413/12 , C07D417/12 , C07D491/04 , C07D491/044 , C07D239/42 , C07C67/327
CPC分类号： C07D405/06 , C07D221/16 , C07D319/06 , C07D405/12 , C07D413/12 , C07D417/12 , C07D491/04
摘要： A process is provided for preparing chiral diol sulfones of the structure where R3 is preferably where R4a is preferably aryl such as phenyl, and R1a is preferably alkyl such as t-butyl, which are intermediates used in preparing HMG CoA reductase inhibitors.
摘要翻译：提供了制备结构的手性二醇砜的方法，其中R3优选在其中，R4a优选为芳基如苯基，R 1a优选为烷基，如叔丁基，其为用于制备HMG CoA还原酶抑制剂的中间体。

8. 发明授权

US06806381B2 Process for the preparation of aniline-derived thyroid receptor ligands 失效
标题翻译：制备苯胺衍生甲状腺受体配体的方法
公开(公告)号：US06806381B2
公开(公告)日：2004-10-19
申请号：US10273268
申请日：2002-10-17
申请人： Ramakrishnan Chidambaram , Joydeep Kant , Raymond E. Weaver , Jurong Yu , Arun Ghosh
发明人： Ramakrishnan Chidambaram , Joydeep Kant , Raymond E. Weaver , Jurong Yu , Arun Ghosh
IPC分类号： C07C22900
CPC分类号： C07C309/65 , C07C45/00 , C07C201/12 , C07C205/12 , C07C205/37 , C07C205/38 , C07C205/43 , C07C213/02 , C07C231/02 , C07C233/25 , C07C309/24 , C07C47/575 , C07C217/90
摘要： Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.
摘要翻译：提供了合成苯胺衍生物的方法，特别是具有作为甲状腺受体配体活性的某些苯胺衍生物。

9. 发明授权

US06353120B2 Process for the preparation of a paclitaxel C-4 methyl carbonate analog 失效
标题翻译：紫杉醇C-4甲基碳酸酯类似物的制备方法
公开(公告)号：US06353120B2
公开(公告)日：2002-03-05
申请号：US09813085
申请日：2001-03-20
申请人： Joydeep Kant
发明人： Joydeep Kant
IPC分类号： C07D30514
CPC分类号： C07D305/14 , C07F7/1804
摘要： A process for the synthesis of a C-4 methyl carbonate paclitaxel analog from 10-deacetylbaccatin III by the selective reduction of the acetate at the C-4 position of 10-deacetylbaccatin using Red-Al.
摘要翻译：通过使用Red-Al在10-脱乙酰基浆果赤霉素的C-4位选择性还原乙酸酯来合成来自10-脱乙酰基浆果赤霉素III的C-4甲基碳酸酯紫杉醇类似物的方法。

10. 发明授权

US07956214B2 Process for the preparation of aniline-derived thyroid receptor ligands 失效
标题翻译：制备苯胺衍生甲状腺受体配体的方法
公开(公告)号：US07956214B2
公开(公告)日：2011-06-07
申请号：US12456313
申请日：2009-06-15
申请人： Ramakrishnan Chidambaram , Joydeep Kant , Raymond E. Weaver , Jurong Yu , Arun Ghosh
发明人： Ramakrishnan Chidambaram , Joydeep Kant , Raymond E. Weaver , Jurong Yu , Arun Ghosh
IPC分类号： C07C309/00
CPC分类号： C07C309/65 , C07C45/00 , C07C201/12 , C07C205/12 , C07C205/37 , C07C205/38 , C07C205/43 , C07C213/02 , C07C231/02 , C07C233/25 , C07C309/24 , C07C47/575 , C07C217/90
摘要： Provided are processes for the synthesis of aniline derivatives, specifically certain aniline derivatives which have activity as thyroid receptor ligands.
摘要翻译：提供了合成苯胺衍生物的方法，特别是具有作为甲状腺受体配体活性的某些苯胺衍生物。

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