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    • 1. 发明授权
    • 12,13-(피라노실)-인돌로[2,3-a]피롤로[3,4-c]카르바졸및 12,13-(피라노실)-푸로[3,4-c]인돌로[2,3-a]카르바졸화합물, 이들의 제조 방법 및 이들을 함유하는 약제학적조성물
    • 12,13-(피라노실) - 인돌로[2,3-a]피롤로[3,4-c]카르바졸및12,13-(피라노실) - 푸로[3,4-c]인돌로[ 2,3-a]카르바졸화합물,이들의제조방법및이들을함유하는약제학적조성물
    • KR100453980B1
    • 2004-10-20
    • KR1020000068432
    • 2000-11-17
    • 르 라보레또레 쎄르비에르
    • 프루도메,미첼르모로,파스칼아니존,패브리스마르미농,크리스텔르아타시,과넴피에르,알랭프페이페르,브루노레나르드,피에르
    • C07D209/82
    • C07H19/23
    • A composition comprises 12,13-(Pyranosyl)-indolo(2,3-a)pyrrolo(3,4-c)carbazole and 12,13-(pyranosyl)-furo(3,4-c)indolo(2,3-a)carbazole derivatives (I), or their isomers, salts with acids or bases, are new A composition comprises 12,13-(Pyranosyl)-indolo(2,3-a)pyrrolo(3,4-c)carbazole and 12,13-(pyranosyl)-furo(3,4-c)indolo(2,3-a)carbazole derivatives of formula (I), or their isomers, salts with acids or bases, are new R1, R2 = U-V; U = 1-6C alkylene, optionally substituted by one or more halo or OH, and which may be unsaturated; V = H, halo, CN, NO2, N3, 1-6C alkyl, aryl, arylalkyl, OH, 1-6C alkoxy, aryloxy, aryl alkoxy, formyl, carboxy, aminocarbonyl, NRaRb, -CO-T1, -CO-NRa-T1, -NRa-CO-T1, -O-CO-T1, -CO-O-T1, -O-T2-NRaRb, -OT2-ORa, -O-T2-COORa, -NRa-T2-NRaRb, -NRa-T2-ORa, -NRa-T2-CO2Raor S(O)n-Ra; Ra, Rb = H, 1-6C alkyl, aryl, or arylalkyl, or both together with the N atom form a 5-7 membered heterocycle which may contain a second heteroatom (O or N) and may be substituted by alkyl, alkoxy, OH, amino, 1-6C alkylamino, or 1-6C dialkylamino; T1 = 1-6C alkyl, aryl, 1-6C arylalkyl, 1-6C alkylene, optionally substituted by -ORa, -NRaRb, -COORa, -CO-Ra, or -CO-NRaRb; T2 = 1-6C alkylene; n = 0 - 2; G = O or NR3; R3 = H, 1-6C alkyl, aryl, arylalkyl, cycloalkyl, cycloalkyl alkyl, -ORa, -NRaRb, -OT2-NRaRb, -NRa-T2-NRaRb, 1-6C hydroxylamino, dihydroxylamino, -CO-Ra, -NH-CO-Ra, 1-6C alkylene, optionally substituted by one or more of halogen, CN, NO2, -ORa, -NRaRb, -COORa, -CORa, hydroxylamino, dihydroxylamino, or -CO-NHRa; X = H, OH, 1-6C alkoxy, SH, or 1-6C alkylthio; Y = H, or X and Y together with the C atom form carbonyl; X1 = H, OH, 1-6C alkoxy, SH, or 1-6C alkylthio; Y1 = H or X1 and Y1 together with the C atom form carbonyl; R4, R5 = H, halogen, OH, alkoxy, aryloxy, aryl alkoxy, alkyl, arylalkyl, aryl, amino (optionally substituted by one or two alkyl, alkyl, aryl and arylalkyl groups), azido, -N=NRa, or -O-CO-Rc; Rc = 1-6C alkyl (optionally substituted by one or more halogen, OH, amino, alkylamino and dialkylamino groups), aryl, aralkyl, cycloalkyl or heterocycloalkyl; R6 = -U1-R4; U1 = a bond or methylene; or R4, R5, and R6 taken in pairs together with the C atoms may = 3-6 membered ring containing 1 or 2 O atoms, except for the following specific compounds: 1,11-dichloro-12,13-(1,2-(4-(O-methyl- beta -D-mannopyranosyl))-6,7,12,13-tetrahydro(5H)indolo(2,3-a)pyrrolo(3,4-c )carbazole-5,7-dio ne; 12,13-(1,2-(4-(O-methyl- beta -D-mannopyranosyl))-6,7,12,13-tetrahydro(5H)indolo(2,3-a)pyrrolo(3,4-c )carbazole-5,7-dione; 12,13-(1,2-(4-(O-methyl- beta -D-mannopyranosyl))-6,7,12,13-tetrahydro(5H)indolo(2,3-a)pyrrolo(3,4-c )carbazole-5-one; and 12,13-(1,2-(4-(O-methyl- beta -D-mannopyranosyl))-5,6,12,13-tetrahydro(7H)indolo(2,3-a)pyrrolo(3,4-c )carbazole-7-one.
    • 组合物包含12,13-(吡喃糖基) - 吲哚并(2,3-a)吡咯并(3,4-c)咔唑和12,13-(吡喃糖基) - 呋喃并(3,4-c)吲哚并 -a)咔唑衍生物(I)或其异构体,与酸或碱形成的盐是新的。组合物包含12,13-(吡喃糖基) - 吲哚并(2,3-a)吡咯并(3,4-c)咔唑和 式(I)的12,13-(吡喃糖基) - 呋喃并(3,4-c)吲哚并(2,3-a)咔唑衍生物或其异构体,与酸或碱的盐是新的R 1,R 2 = U = 1-6C亚烷基,任选被一个或多个卤素或OH取代,并且其可以是不饱和的; 卤素,CN,NO2,N3,1-6C烷基,芳基,芳基烷基,OH,1-6C烷氧基,芳氧基,芳基烷氧基,甲酰基,羧基,氨基羰基,NRaRb,-CO-T1,-CO-NRa -NRa-CO-T1,-O-CO-T1,-CO-O-T1,-O-T2-NRaRb,-OT2-ORa,-O-T2-COORa,-NRa-T2-NRaRb, -NRa-T2-ORa,-NRa-T2-CO2Ra或S(O)n-Ra; Ra,Rb = H,1-6C烷基,芳基或芳基烷基或二者与N原子一起形成5-7元杂环,其可以含有第二个杂原子(O或N)并可以被烷基,烷氧基, OH,氨基,1-6C烷基氨基或1-6C二烷基氨基; 任选地被-ORa,-NRaRb,-COORa,-CO-Ra或-CO-NRaRb取代的T1 = 1-6C烷基,芳基,1-6C芳基烷基,1-6C亚烷基; T2 = 1-6C亚烷基; n = 0-2; G = O或NR3; R3 = H,1-6C烷基,芳基,芳基烷基,环烷基,环烷基烷基,-ORa,-NRaRb,-OT2-NRaRb,-NRa-T2-NRaRb,1-6C羟基氨基,二羟基氨基, 任选地被一个或多个卤素,CN,NO 2,-OR a,-NR a R b,-COOR a,-COR a,羟基氨基,二羟基氨基或-CO-NHR a取代的-CO-R a, X = H,OH,1-6C烷氧基,SH或1-6C烷硫基; Y = H,或者X和Y与C原子一起形成羰基; X1 = H,OH,1-6C烷氧基,SH或1-6C烷硫基; Y1 = H或X1和Y1与C原子一起形成羰基; (其任选被一个或两个烷基,烷基,芳基和芳基烷基取代),叠氮基,-N = NRa或 - O-CO-RC; Rc = 1-6C烷基(任选被一个或多个卤素,OH,氨基,烷基氨基和二烷基氨基取代),芳基,芳烷基,环烷基或杂环烷基; R6 = -U1-R4; U1 =键或亚甲基; 或与C原子一起成对取代的R 4,R 5和R 6可以=含有1或2个O原子的3-6元环,除了以下具体化合物:1,11-二氯-12,13-(1,2 - (4-(O-甲基-β-D-吡喃甘露糖基))-6,7,12,13-四氢(5H)吲哚并(2,3-a)吡咯并(3,4-c)咔唑-5,7 - 二烯; 12,13-(1,2-(4-(O-甲基-β-D-吡喃甘露糖基))-6,7,12,13-四氢(5H)吲哚并(2,3-a)吡咯并 (3,4-c)咔唑-5,7-二酮; 12,13-(1,2-(4-(O-甲基-β-D-吡喃甘露糖基))-6,7,12,13-四氢( 5H)吲哚并(2,3-a)吡咯并(3,4-c)咔唑-5-酮和12,13-(1,2-(4-(O-甲基-β-D-吡喃甘露糖基)) - 5,6,7,13-四氢(7H)吲哚并(2,3-a)吡咯并(3,4-c)咔唑-7-酮。
    • 2. 发明公开
    • 벤조[b]피라노[3,2-h]아크리딘-7-온 화합물, 이의 제조방법 및 이를 함유하는 약제 조성물
    • BENZO B | PYRANO(3,2-H)ACRIDIN-7-ONE的新衍生物,其制备方法和含有该衍生物的药物化合物
    • KR1020030010513A
    • 2003-02-05
    • KR1020020043537
    • 2002-07-24
    • 르 라보레또레 쎄르비에르
    • 코흐,미쉘틸레퀸,프랑소와즈미쉘,실비에세구인,엘리자베스엘옴리,아브델하킴히크만,존피에르,알라인페이페르,브루노레나르드,피에르
    • C07D491/048
    • C07D491/04
    • PURPOSE: Provided are new benzo(b)pyrano(3,2-h)acridin-7-one compounds, their isomers and N-oxides, and addition salts thereof with a pharmaceutically acceptable acid or base, and medicinal products containing the same which are useful in the treatment of cancer. CONSTITUTION: A new benzo(b)pyrano(3,2-h)acridin-7-one compound is selected from those of formula(I), wherein: X and Y represent group selected from hydrogen, halogen, mercapto, cyano, nitro, alkyl, trihaloalkyl, trihaloalkylcarbonylamino, -ORa, -NRaRb, -NRa-C(O)-T1, -O-C(O)-T1, -O-T2-NRaRb, -O-T2ORa, -NRa-T2NRaRb, -NRa-T2-ORa and -NRa-T2-CO2Ra wherein Ra, Rb, T1, T2 are as defined in the specification, or X and Y together form a methylenedioxy or ethylenedioxy, R1 represents hydrogen or alkyl, R2 represents a group selected from hydrogen, -ORa, -NRaRb, -NRa-C(O)-T1, -O-C(O)-T1, -O-T2-NRaRb, -O-T2-ORa, -NRa-T2-NRaRb, -NRa-T2-ORa and -NRa-T2-CO2Ra wherein Ra, Rb, T1 and T2 are as defined hereinbefore, R3 and R4 represent hydrogen or alkyl, W represents a group of formula -CH(R5)-CH(R6)-, -CH=C(R7)-, -C(R7)=CH- or -C(O)-CH(R8)- wherein R5, R6, R7 and R8 are as defined in the specification.
    • 目的:提供新的苯并(b)吡喃并(3,2-h)吖啶-7-酮化合物,其异构体和N-氧化物及其与药学上可接受的酸或碱的加成盐,以及含有它们的药物 可用于治疗癌症。 构成:新的苯并(b)吡喃并(3,2-h)吖啶-7-酮化合物选自式(I)的化合物,其中:X和Y表示选自氢,卤素,巯基,氰基,硝基 ,烷基,三卤代烷基,三卤代烷基羰基氨基,-ORa,-NRaRb,-NRa-C(O)-T1,-OC(O)-T1,-O-T2-NRaRb,-O-T2ORa,-NRa-T2NRaRb, -T2-ORa和-NRa-T2-CO2Ra,其中Ra,Rb,T1,T2如说明书中所定义,或X和Y一起形成亚甲二氧基或亚乙二氧基,R 1表示氢或烷基,R 2表示选自氢 ,-ORa,-NR a R b,-NR a -C(O)-T1,-OC(O)-T1,-O-T 2 -NR a R b,-O-T 2 -OR a,-NR a -T 2 -NR a R b,-NR a -T 2 -ORa和-NR a -T 2 -CO 2 R a其中R a,R b,T 1和T 2如上所定义,R 3和R 4表示氢或烷基,W表示式-CH(R 5)-CH(R 6) - , - CH = C(R 7) - , - C(R 7)= CH-或-C(O)-CH(R 8) - ,其中R 5,R 6,R 7和R 8如说明书中所定义。
    • 3. 发明公开
    • 치환된 피리딘 또는 피페리딘 화합물, 이들의 제조 방법및 이들을 함유하는 약제 조성물
    • 新替代的吡啶或哌啶化合物,其生产和含有该组合物的药物组合物
    • KR1020010020808A
    • 2001-03-15
    • KR1020000023682
    • 2000-05-03
    • 르 라보레또레 쎄르비에르
    • 메스-촌,오토유,추-이레스타게,피에르레브룬,마리에-세실사이그나르드,다니엘-헨리레나르드,피에르
    • C07D211/00
    • C07D213/30C07D211/22C07D211/32C07D213/36C07D213/50
    • PURPOSE: A compound is provide which exhibits an analgesic characteristic and a characteristic promoting recognizing process and useful for treatment of pain and treatment of aging of brain and amnesia accompanying neurodegeneration diseases such as Alzheimer's disease, Parkinson's disease and Pick disease. CONSTITUTION: The compound is represented by formula I (A is pyridine or the like; R3 is hydroxy for the like; R4 is phenyl or the like; R1 is H or the like; R5 is a 5-6 membered heterocycle which may contain a nitrogen atom binding to the ring A and may contain another hetero atom selected from sulfur, oxygen and nitrogen; R6 is H or the like), e.g. 1-(4-bromophenyl)-2-(1-methyl-2- piperidinyl)-1-ethanone. The compound of formula I is obtained by reacting, e.g. a compound obtained by alkylating a compound of formula II (X is H or fluorine) with an alkylating agent with a compound of formula III (Ra and Rb form a 5 to 6-membered heterocycle which may contain another hetero atom selected from sulfur, oxygen or nitrogen together with nitrogen binding to these groups; Rc is H or the like).
    • 目的:提供一种化合物,其具有镇痛特征和特征促进识别方法,并且可用于治疗伴随神经变性疾病如阿尔茨海默病,帕金森病和皮克病的脑和遗忘症的疼痛和治疗老化。 构成:该化合物由式I表示(A为吡啶等; R3为羟基等; R4为苯基等; R1为H等; R5为5-6元杂环,可含有 氮原子与环A结合并且可以含有选自硫,氧和氮的另外的杂原子; R 6是H等),例如 1-(4-溴苯基)-2-(1-甲基-2-哌啶基)-1-乙酮。 式I的化合物是通过使例如 通过烷基化剂与式III化合物(R a和R b形成5至6元杂环,其可以含有选自硫,氧的另外的杂原子)将式II化合物(X为H或氟)烷基化得到的化合物 或氮与氮结合这些基团; R c是H等)。
    • 5. 发明授权
    • 아미노피롤린 화합물, 이의 제조 방법 및 이를 함유하는약제 조성물
    • 아미노피롤린화합물,이의제조방법및이를함유하는약제조성물
    • KR100453981B1
    • 2004-10-20
    • KR1020000068434
    • 2000-11-17
    • 르 라보레또레 쎄르비에르
    • 부께,빠스깔에하르,쟝-다니엘브뤼방,베로니끄펠드망,죠지안느샨,스테판스깔베르,엘리자베스프페이페르,브루노레나르드,피에르
    • C07D207/09
    • C07D207/14C07D209/40
    • 2-Cyclopropylhydrocarbylamino-pyrrolidine derivatives (I) are new. 2-Cyclopropylhydrocarbylamino-pyrrolidine derivatives of formula (I) and their isomers and salts are new: n = 1 or 2; X = 1-6C alkylene, 2-6C alkenylene (containing 1-3 double bonds), 2-6C alkynylene (containing 1-3 triple bonds) or optionally Q-substituted arylene or heteroarylene; R10, R12 = H or 1-6C alkyl; R11 = H; or R10+R11 or R11+R12 = a bond; R2-R4 = H, 1-6C alkyl, 1-6C hydroxyalkyl, 1-6C alkoxy, 2-7C alkoxycarbonyl or optionally Q-substituted aryl, aryl(1-6C)alkyl or aryloxy(1-6C)alkyl, or two of R2-R4 form a 5-7C cycloalkane ring; Q = halogen, 1-6C alkyl, 1-6C alkoxy, OH, CN, NO2, NH2 and/or mono- or di(1-6C alkyl)amino; aryl = phenyl or naphthyl; arylene = phenylene or naphthylene; and heteroaryl and heteroarylene = 4- to 11-membered mono- or bicyclic saturated or partially unsaturated groups containing 1-5 heteroatoms selected from N, O and S. An Independent claim is also included for a process for preparing compounds (I).
    • 2-环丙基烃基氨基 - 吡咯烷衍生物(I)是新的。 式(I)的2-环丙基烃基氨基 - 吡咯烷衍生物及其异构体和盐是新的:n = 1或2; X = 1-6C亚烷基,2-6C亚烯基(包含1-3个双键),2-6C亚炔基(包含​​1-3个三键)或任选地Q-取代的亚芳基或杂亚芳基; R10,R12 = H或1-6C烷基; R11 = H; 或R10 + R11或R11 + R12 =键; R2-R4 = H,1-6C烷基,1-6C羟烷基,1-6C烷氧基,2-7C烷氧羰基或任选被Q取代的芳基,芳基(1-6C)烷基或芳氧基(1-6C)烷基或两 的R2-R4形成5-7C环烷烃环; Q =卤素,1-6C烷基,1-6C烷氧基,OH,CN,NO 2,NH 2和/或单 - 或二(1-6C烷基)氨基; 芳基=苯基或萘基; 亚芳基=亚苯基或亚萘基; 和杂芳基和杂亚芳基=含有1-5个选自N,O和S的杂原子的4-至11-元单 - 或双环饱和或部分不饱和基团。还包括独立权利要求用于制备化合物(I)的方法。