CN1224350A - 托吡酯或其衍生物在制备治疗躁狂抑郁性两极(神经)细胞失调症的药剂中的用途 - Google Patents

托吡酯或其衍生物在制备治疗躁狂抑郁性两极(神经)细胞失调症的药剂中的用途 Download PDF

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CN1224350A
CN1224350A CN97195907A CN97195907A CN1224350A CN 1224350 A CN1224350 A CN 1224350A CN 97195907 A CN97195907 A CN 97195907A CN 97195907 A CN97195907 A CN 97195907A CN 1224350 A CN1224350 A CN 1224350A
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Abstract

本发明公开了用于治疗躁狂抑郁症的抗惊厥药物衍生物。

Description

托吡酯或其衍生物在制备治疗躁狂抑郁性 两极(神经)细胞失调症的药剂中的用途
本发明的背景技术
式Ⅰ化合物是结构上新颖的抗癫痫化合物，
Figure A9719590700031
动物实验表明它是高效的抗惊厥剂(Maryanoff,B.E,Nortey,S.O.,Gardocki,J.F.,Shank,R.P.和Dodgson,S.P.，《医药化学杂志》(J.Med.Chem.)30,880-887,1987；Maryanoff,B.E.,Costanzo,M.J.,Shank,R.P.,Schupsky,J.J.,Ortegon,M.E.,和Vaught J.L.《生物有机与医药化学快报》(Bioorganic & MedicianalChemistry Letters)3,2653-2656,1993,McComsey,D.F.和Maryanoff,B.E.，《有机化学杂志》(J.Org.Chem.)1995)。这些化合物包含在Nos.4,513,006、5,384,327和5,498,629三项美国专利中。已证实这些化合物其中之一2,3∶4,5-二O-(1-甲基亚乙基)-β-D-吡喃果糖氨基磺酸酯，即称为托吡酯者，在人类癫痫病的临床试验中，它在治疗简单与复杂的部分癫痫发作和继发性全身癫痫发作方面，可作为有效的辅助疗法或单一疗法(E.FAUGHT,B.J.WILDER,R.E.RAMSEY,R.A.REIFE,LD.KRAMER,G.W.PLEDGER,R.M.KARIM等，《癫痫》36(S4)33,1995；S.K.SACHDEO,R.C.SACHDEO,R.A.REIFE,P.LIM和G.PLEDGER，《癫痫》36(S4)33,1995)，在英国、芬兰、美国和瑞典已广泛销售，用于治疗伴有或不伴继发性全身癫痫发作的简单和复杂的部分癫痫发作的癫痫，并已在全世界许多国家提出希望获得法定批准的申请。
最初是在传统的小鼠最大电休克癫痫发作(MES)实验中发现式Ⅰ化合物具有抗惊厥活性的(SHANK,R.P.GARDOCKI,J.F.,VAUGHT,J.L.,DAVIS,CB.,SCHUPSKY,J.J.,RAFFA,R.B.,DODGSON,S.J.,NORTEY,S.O.,和MARYANOFF,B.E.，《癫痫》35,450-460,1994)。随后的研究证实了式Ⅰ化合物在大鼠MES实验中也是非常有效的。而且最近发现托吡酯在一些癫痫的啮齿动物模型中能有效地阻止癫痫发作(J.NAKAMURA,S.TAMURA,T.KANDA,A.ISHII,K.ISHIHARA,T.SERIKAWA,J.YAMADA和M.SASA，《欧洲药学杂志》，254,83-89,1994)，并在一种激动致癫痫的动物模型中也能阻断癫痫发作(A.WAUQUIER和S.ZHOU，《癫痫研究》，24,73-77,1996版)。
有关托吡酯的最近临床前研究揭示了其以前未被发现的药学性质，这提示托吡酯在治疗躁狂抑郁性两极(神经)细胞失调症(MDBD)方面是有效的。
对本发明的说明
因此，已发现下式Ⅰ化合物可用于治疗躁狂抑郁性两极(神经)细胞失调症(MDBD)。式Ⅰ中X是O或CH2，对R1、R2、R3、R4、R5的定义如后所述。
Figure A9719590700041
对优选实施方式的详细描述
本发明的氨基磺酸酯有以下式(Ⅰ)的结构：
Figure A9719590700042
其中
X是CH2或氧；
R1是氢或烷基；和
R2、R3、R4和R5各自独立地是氢或低级烷氧基，当X是氧时，R2和R3和/或R4和R5可以一起是如下式(Ⅱ)的亚甲二氧基
Figure A9719590700051
其中
R6和R7是相同或不同的，可以是氢、低级烷基或是烷基，并且可结合形成环戊基或环己基环。
尤其是，R1是氢或具约1-4个碳原子的烷基，如甲基、乙基和异丙基。此说明书中的烷基包括直链和支链烷基。R2、R3、R4、R5、R6和R7代表的烷基基团约有1-3个碳原子，包括甲基、乙基、异丙基和正丙基。
式(Ⅰ)一组特别的化合物是，其中X是氧，R2和R3与R4和R5均为具有式(Ⅱ)结构的亚甲二氧基，其中R6和R7均为氢、烷基，或结合形成一螺环戊基或环己基环，尤其是R6和R7均为烷基，如甲基。第二组化合物是那些X为CH2、R4和R5结合形成苯环者。第三组式(Ⅰ)化合物是那些R2和R3均为氢者。
可以按以下方法合成式(Ⅰ)化合物：
(a)将具有结构式为RCH2OH的醇与具有结构式为ClSO2NH2或ClSO2NHR1的氯氨基磺酸酯在有碱如丁醇钾(potassium a-butoxide)或氢化钠存在的条件下进行反应，反应温度约为-20℃-25℃，反应溶剂为甲苯、四氢呋喃(THF)或二甲基甲酰胺，其中R是下式(Ⅲ)的一部分。
Figure A9719590700052
(b)将具有结构式RCH2OH的醇与具有结构式SO2Cl2的硫酰氯在有碱如三乙胺或吡啶存在的条件下反应，反应温度约为-40℃至25℃，反应溶剂为二乙醚或二氯甲烷，生成具有结构式RCH2OSO2Cl的氯硫酸酯。
然后可将具有式RCH2OSO2Cl的氯硫酸酯与具有式R1NH2的胺在约40℃至25℃的温度条件下、在溶剂如二氯甲烷或乙腈中反应生成式(Ⅰ)化合物。(b)反应的条件在T.Tsuchiya等，Tet.Letters,No.36,3365-3368页(1978)有记载。
(c)按M.Hedayatullah在Tet.Letters,2455-2458(1975)所记载的，将氯硫酸酯RCH2OSOCl与金属叠氮化物如叠氮化钠在溶剂如二氯甲烷或乙腈中反应，产生叠氮硫酸酯，式为RCH2OSO2N3。然后将叠氮硫酸酯还原成具有式(Ⅰ)的化合物，其中R1是由催化氢化作用产生的氢，如，一种贵重金属和H2的催化氢化反应，或通过将铜金属在如甲醇的溶剂中加热产生的。
具有式RCH2OH结构的初始物质可以通过市售得到或按本领域已知的方法得到。例如，具有式RCH2OH结构的初始物质(其中R2和R3、与R4和R5相同且具有式(Ⅱ)结构)，可以按R.F.Brady在《碳水化合物研究》，14卷，35-40页(1970)所述的方法得到，或通过将具有R6COR7酮或醛结构的三甲基硅烯醇醚与果糖在约25℃条件下、在卤化碳类溶剂如二氯甲烷中、在有质子酸如盐酸或路易斯酸如氯化锌存在下反应而得到。G.L.Larson等在《有机化学杂志》38卷22期3935页(1973)记载了三甲基硅烯醇醚反应。
进而，可以采用标准还原技术，如与氢化锂铝、硼氢化钠或甲硼烷-THF配合物在惰性溶剂如二甘醇二甲醚、四氢呋喃或甲苯中，在约为0℃至100℃的温度下反应，如H.O.House在《现代合成反应》，第2版，45-144页(1972)所述，将具有式RCHOH和RCHO结构的羧酸和醛还原成式RCH2OH结构的化合物。
也可以通过美国专利NO.4,513,006公开的方法制备式Ⅰ化合物，此专利在此作为参考。
式Ⅰ化合物包括各种单独的异构体及其外消旋物，如，6元环上的R2、R3、R4和R5的各种α-和β-侧链，即在附图平面的上方和下方。优选亚甲二氧基基团(Ⅱ)中的氧连接在6元环的同一侧。
躁狂抑郁性两极(神经)细胞失调症是一种病因未知的进行性精神疾病(F.GOODWIN和K.R.JAMISON，《躁狂抑郁性疾病》，牛津大学出版社，纽约，1990)；但躁狂抑郁性疾病的复发假想是由电生理激发造成的(F.GOODWIN和K.R.JAMISON，《躁狂抑郁性疾病》，牛津大学出版社，纽约，P405-407,1990)。已证明托吡酯在阻断大鼠的激动性癫痫发作方面是有效的。(A.WAUQUIER和S.ZHOU，《癫痫研究》，24,73-77,1996年出版)。
为治疗躁狂抑郁性两极(神经)细胞失调症，对一般的成年人可以按约50到200mg范围的每日剂量使用式(Ⅰ)化合物，通常将此剂量分为两次服用。每单位剂量应含有约25到100mg的活性成分。
为制备此项发明中的药物化合物，将一种或多种具有式(Ⅰ)结构的氨基磺酸酯化合物按照常规的药物配制技术与药物载体紧密掺合，其中，根据用药所需的剂型，如口服、或栓剂或肠胃外剂型可以采用多种形式的载体。在制备口服剂型的组合物时，可以使用任何一种常用药物介质。因此，对于口服液体制剂，例如悬孚剂、酏剂和溶液剂，合适的载体和添加剂包括水、乙二醇、油、乙醇、调味剂、防腐剂、着色剂和类似物质；对于固体口服制剂，如粉剂、胶囊和药片，合适的载体和添加剂包括淀粉、糖、稀释剂、制粒剂、润滑剂、粘合剂、崩解剂和类似物质。由于药片和胶囊服用方便，它们代表了最有利的口服单剂量剂型，在这种情况下显然使用了固体药物载体。如果需要，药片可以采用标准工艺包覆糖衣或肠溶衣。可以使用可可脂作为载体制备栓剂。对于肠胃外剂型，载体通常包括无菌水，而为了如助溶或保存的目的，也可以包括其它成分。也可以使用适宜的液体载体、悬浮剂和类似物质，制备注射用悬浮剂。托吡酯通常采用含有25mg、100mg或200mg活性成分的圆形片剂口服用药。此药片中含有下列非活性组分：含水乳糖、预胶化淀粉、微晶纤维素、甘醇酸定粉钠、硬脂酸镁、纯化水、巴西棕榈蜡、羟丙基甲基纤维素、二氧化钛、聚乙二醇、合成氧化铁和多乙氧基醚。
此处的药物组合物如药片、胶囊、粉针剂、茶剂、栓剂和类似剂型，每剂量单位将含有大约25到100mg的活性成分。

Claims (4)

1．一种治疗躁狂抑郁性两极(神经)细胞失调症的方法，包括给患此病的哺乳动物服用有效量的治疗此病的式Ⅰ化合物：其中
X是CH2或氧；
R1是氢或烷基；和
R2、R3、R4和R5各自独立地是氢或低级烷基，当X是氧时，R2和R3和/或R4和R5可以一起是如下式(Ⅱ)的亚甲二氧基
Figure A9719590700022
其中
R6和R7是相同或不同的，可以是氢、低级烷基或是烷基，且可结合形成环戊基或环己基环。
2．根据权利要求1所述的方法，其中式Ⅰ化合物是托吡酯。
3．根据权利要求1所述的方法，其中治疗有效量是约50-200mg。
4．根据权利要求1所述的方法，其中所述的量是约25-100mg。
CN97195907A 1996-06-28 1997-06-24 托吡酯或其衍生物在制备治疗躁狂抑郁性两极(神经)细胞失调症的药剂中的用途 Pending CN1224350A (zh)

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Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE261724T1 (de) * 1998-11-17 2004-04-15 Ortho Mcneil Pharm Inc Antikonvulsive derivate zur behandlung von posttraumatischen stresserkrankungen
US20020006908A1 (en) * 1998-12-03 2002-01-17 Daniel P. Van Kammen Anticonvulsant derivatives useful in treating schizophrenia
WO2000045812A1 (en) 1999-02-08 2000-08-10 Ortho-Mcneil Pharmaceutical, Inc. Anticonvulsant derivatives useful in treating autism
ATE294577T1 (de) * 1999-02-24 2005-05-15 Univ Cincinnati Verwendung von sulfamat derivaten zur behandlung von impulsiven störungen
NZ514813A (en) * 1999-04-08 2004-12-24 Ortho Mcneil Pharm Inc Anticonvulsant derivatives useful in treating chronic neurodegenerative disorders
US6420369B1 (en) 1999-05-24 2002-07-16 Ortho-Mcneil Pharmaceutical, Inc. Anticonvulsant derivatives useful in treating dementia
US7553818B2 (en) * 1999-06-14 2009-06-30 Vivus, Inc. Combination therapy for effecting weight loss and treating obesity
US20080255093A1 (en) * 1999-06-14 2008-10-16 Tam Peter Y Compositions and methods for treating obesity and related disorders
US7659256B2 (en) * 1999-06-14 2010-02-09 Vivus, Inc. Combination therapy for effecting weight loss and treating obesity
US7056890B2 (en) 1999-06-14 2006-06-06 Vivus, Inc. Combination therapy for effecting weight loss and treating obesity
US7674776B2 (en) 1999-06-14 2010-03-09 Vivus, Inc. Combination therapy for effecting weight loss and treating obesity
EP1187603B1 (en) 1999-06-14 2007-08-08 Vivus, Inc. Combination therapy for effecting weight loss and treating obesity
US20080103179A1 (en) * 2006-10-27 2008-05-01 Tam Peter Y Combination Therapy
US6191117B1 (en) * 2000-07-10 2001-02-20 Walter E. Kozachuk Methods of producing weight loss and treatment of obesity
MXPA03001001A (es) 2000-08-02 2003-10-14 Johnson & Johnson Derivados anticonvulsionantes utiles para el tratameinto de la depresion.
EP1345602B1 (en) 2000-11-30 2010-07-21 Novodermix International Limited Wound healing
EP1423127A1 (en) * 2001-08-30 2004-06-02 Ortho-Mcneil Pharmaceutical, Inc. Treatment of dementia and memory disorders with anticonvulsants and acetylcholinesterase inhibitors
EP1438036A2 (en) * 2001-10-12 2004-07-21 Eli Lilly And Company Use of sulfonamide derivatives as pharmaceuticals compounds
US7790905B2 (en) * 2002-02-15 2010-09-07 Mcneil-Ppc, Inc. Pharmaceutical propylene glycol solvate compositions
US7927613B2 (en) 2002-02-15 2011-04-19 University Of South Florida Pharmaceutical co-crystal compositions
US20100311701A1 (en) * 2002-02-15 2010-12-09 Transform Pharmaceuticals, Inc Pharmaceutical Co-Crystal Compositions
US20050025791A1 (en) * 2002-06-21 2005-02-03 Julius Remenar Pharmaceutical compositions with improved dissolution
US6559293B1 (en) * 2002-02-15 2003-05-06 Transform Pharmaceuticals, Inc. Topiramate sodium trihydrate
US20090088443A1 (en) * 2002-02-15 2009-04-02 Julius Remenar Novel crystalline forms of conazoles and methods of making and using the same
JP4906233B2 (ja) * 2002-03-01 2012-03-28 ユニバーシティー オブ サウス フロリダ 少なくとも１種の有効薬剤成分を含有する多構成要素固相
US20070059356A1 (en) * 2002-05-31 2007-03-15 Almarsson Oern Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
WO2004010970A1 (en) * 2002-07-29 2004-02-05 Alza Corporation Formulations and dosage forms for controlled delivery of topiramate
US8183290B2 (en) 2002-12-30 2012-05-22 Mcneil-Ppc, Inc. Pharmaceutically acceptable propylene glycol solvate of naproxen
WO2005000294A1 (en) * 2003-06-06 2005-01-06 Pharmacia Corporation Selective inhibitor and an anticonvulsant agent for the treatment of central nervous system disorders
JP2007517063A (ja) * 2003-12-29 2007-06-28 アルザ・コーポレーシヨン トピラメートの新規な薬剤組成物および剤形
MY147767A (en) * 2004-06-16 2013-01-31 Janssen Pharmaceutica Nv Novel sulfamate and sulfamide derivatives useful for the treatment of epilepsy and related disorders
TW200612905A (en) * 2004-06-16 2006-05-01 Janssen Pharmaceutica Nv Novel sulfamate and sulfamide derivatives useful for the treatment of epilepsy and related disorders
KR20070057848A (ko) * 2004-08-24 2007-06-07 얀센 파마슈티카 엔.브이. 항경련제로 유용한 신규 벤조-융합된 헤테로아릴 설파미드유도체
AU2006249577A1 (en) * 2005-05-20 2006-11-30 Janssen Pharmaceutica N.V. Process for preparation of sulfamide derivatives
US8716231B2 (en) * 2005-12-19 2014-05-06 Janssen Pharmaceutica Nv Use of benzo-fused heterocycle sulfamide derivatives for the treatment of pain
US8492431B2 (en) * 2005-12-19 2013-07-23 Janssen Pharmaceutica, N.V. Use of benzo-fused heterocycle sulfamide derivatives for the treatment of obesity
US8497298B2 (en) * 2005-12-19 2013-07-30 Janssen Pharmaceutica Nv Use of benzo-fused heterocycle sulfamide derivatives for lowering lipids and lowering blood glucose levels
US20070155827A1 (en) * 2005-12-19 2007-07-05 Smith-Swintosky Virginia L Use of benzo-fused heterocycle sulfamide derivatives for the treatment of depression
US8691867B2 (en) * 2005-12-19 2014-04-08 Janssen Pharmaceutica Nv Use of benzo-fused heterocycle sulfamide derivatives for the treatment of substance abuse and addiction
US8937096B2 (en) * 2005-12-19 2015-01-20 Janssen Pharmaceutica Nv Use of benzo-fused heterocyle sulfamide derivatives for the treatment of mania and bipolar disorder
US20070155823A1 (en) * 2005-12-19 2007-07-05 Smith-Swintosky Virginia L Use of benzo-fused heterocycle sulfamide derivatives as neuroprotective agents
US20070191449A1 (en) * 2006-02-15 2007-08-16 Smith-Swintosky Virginia L Use of Benzo-Heteroaryl Sulfamide Derivatives for the Treatment of Depression
US20070191450A1 (en) * 2006-02-15 2007-08-16 Smith-Swintosky Virginia L Use of Benzo-Heteroaryl Sulfamide Derivatives for the Treatment of Mania and Bipolar Disorder
US20070191474A1 (en) * 2006-02-15 2007-08-16 Smith-Swintosky Virginia L Use of benzo-fused heterocyle sulfamide derivatives for the treatment of migraine
EP2026790A2 (en) * 2006-05-19 2009-02-25 Janssen Pharmaceutica, N.V. Co-therapy for the treatment of epilepsy and related disorders
US9744137B2 (en) * 2006-08-31 2017-08-29 Supernus Pharmaceuticals, Inc. Topiramate compositions and methods of enhancing its bioavailability
ES2555066T3 (es) 2006-11-17 2015-12-28 Supernus Pharmaceuticals, Inc. Formulaciones de liberación sostenida de topiramato
CN102114002B (zh) 2006-12-04 2016-05-11 苏佩努斯制药公司 托吡酯的增强的立即释放制剂
US20090247616A1 (en) * 2008-03-26 2009-10-01 Smith-Swintosky Virginia L Use of benzo-fused heterocyle sulfamide derivatives for the treatment of anxiety
US20090247617A1 (en) * 2008-03-26 2009-10-01 Abdel-Magid Ahmed F Process for the preparation of benzo-fused heteroaryl sulfamates
US8580298B2 (en) 2008-06-09 2013-11-12 Vivus, Inc. Low dose topiramate/phentermine composition and methods of use thereof
US20090304789A1 (en) 2008-06-09 2009-12-10 Thomas Najarian Novel topiramate compositions and an escalating dosing strategy for treating obesity and related disorders
BRPI0915890A2 (pt) 2008-06-23 2015-11-03 Janssen Pharmaceutica Nv forma cristalina de (2s)-(-)-n-(6-cloro-2,3-di-hidro-benzo[1,4]dioxin-2-ilmetil)-sulfamida
US8815939B2 (en) * 2008-07-22 2014-08-26 Janssen Pharmaceutica Nv Substituted sulfamide derivatives
US8652527B1 (en) 2013-03-13 2014-02-18 Upsher-Smith Laboratories, Inc Extended-release topiramate capsules
US9101545B2 (en) 2013-03-15 2015-08-11 Upsher-Smith Laboratories, Inc. Extended-release topiramate capsules
WO2020104837A1 (en) 2018-11-21 2020-05-28 Rosemont Pharmaceuticals Limited Oral topiramate suspension formulations with extended shelf stability and enhanced bioavailability

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4513006A (en) * 1983-09-26 1985-04-23 Mcneil Lab., Inc. Anticonvulsant sulfamate derivatives
US5384327A (en) * 1992-12-22 1995-01-24 Mcneilab, Inc. Anticonvulsant sorbopyranose sulfamates

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CA2258895A1 (en) 1998-01-08
CZ427798A3 (cs) 1999-08-11
CA2258895C (en) 2006-06-06
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US5753693A (en) 1998-05-19
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