NOVEL BORNEOL DERIVATIVES, METHODS OF MANUFACTURING THEM, AND THEIR PHARMACEUTICAL USE
    1.
    发明申请
    NOVEL BORNEOL DERIVATIVES, METHODS OF MANUFACTURING THEM, AND THEIR PHARMACEUTICAL USE 审中-公开
    新BORNEOLDERIVATE,PROCESS FOR THEIR和制药用

    公开(公告)号:WO1996025392A1

    公开(公告)日:1996-08-22

    申请号:PCT/DE1996000297

    申请日:1996-02-19

    IPC分类号: C07C271/22

    摘要: The invention concerns borneol derivatives of general formula (I), wherein: R represents C(O)-CH(OR )-CH(NR R )-R , C(O)-CH(OR )-CH[NH(C(O)-CH(OR )-CH(NR R )-R )] -R ; R and R are identical or different and the same as R ; R and R are identical or different and the same as R ; R is -C(O)R , -SO2R , -C(O)OR , -C(O)SR , -C(O)NHR , -C(O)NR R , (a), alkyl; R is phenyl; R and R are identical or different and stand for alkyl, cycloalkyl, aryl or aralkyl; R are identical or different and stand for hydrogen, alkyl, aryl, acyl, aralkyl, -SO2R , -P(O) (OH)2; R stands for hydrogen, alkyl, aryl, aralkyl. The invention also concerns salts of the said compounds with physiologically tolerable bases, alpha -, beta - or gamma -cyclodextrine clathrates of the said compounds and compounds of formula (I) encapsulated with liposomes. The compounds are active as tubulin polymerisation antagonists.

    摘要翻译: 本发明betrfifft Borneolderivate通式(I)其中R <1>(O)-CH(OR <6>)C - CH(NR <7A> - [R <7B>) - R的<8>,C(O) -CH(OR <6>) - CH [NH((O)-CH(OR <6B>)C - CH(NR <7A> - [R <7B>) - R的<8>)] - R的<8>, [R <6A>,R <6B>是相同的或不同的并且R <6>,R <7A>,R <7B>是相同的或不同的并且R <7>,R <7> -C(O)R <12>,-SO 2 R <12>,-C(O)OR <12>,-C(O)SR <12>,-C(O)NHR <9D>,-C(O)NR <9D>ř <9A>中,(a)烷基,R <8>是苯基,R ,R <12>是相同的或不同的并且是烷基,环烷基,芳基,芳烷基,R <6>是相同的或不同的,是氢 烷基,芳基,酰基,芳烷基,-SO 2 R <9C>,-P(O)(OH)指2,R <13>为氢,烷基,芳基,芳烷基,以及与生理上可耐受的碱,以及它们的α它们的盐 - ,β - 或伽马-Cyclodextrinclathrate和平均封装有通式(I)的脂质体的化合物。 该化合物作为活性聚合的微管蛋白拮抗剂。

    NOVEL BORNEOL ESTERS, PROCESS FOR THEIR PREPARATION AND THEIR PHARMACEUTICAL USE
    3.
    发明申请
    NOVEL BORNEOL ESTERS, PROCESS FOR THEIR PREPARATION AND THEIR PHARMACEUTICAL USE 审中-公开
    新BORNEO LESTER,PROCESS FOR THEIR和制药用

    公开(公告)号:WO1996032376A1

    公开(公告)日:1996-10-17

    申请号:PCT/EP1996001404

    申请日:1996-03-29

    IPC分类号: C07C271/22

    CPC分类号: C07D303/16

    摘要: The invention concernes borneol esters of general formula (I), in which R means T-C(O)-CH(OR )-CH(NR R )-R , C(O)-CH(OR )-CH[NR (C(O)-CH(OR )-CH(NR R )-R )]-R ; R R are identical or different and means R ; R means hydrogen, A, -C(O)R , -C(O)OR , -C(O)SR , -C(O)NHR , -C(O)NR R , -SO2R , C1-C10 alkyl; R , R are identical or different and mean R ; R means (i), heteroaryl substituted by X , C7-C16 aralkyl, alkyl; A is B-[O-(CH2)t-C(O)]0 or 1-, farnesyl-P(O)(OR )-O-(CH2)t-C(O)-; B means protein kinase-inhibitors or farnesyl protein transferase-inhibitors such as for example farnesyl (ii); and T is a bond, Z or a group (iii). The borneol esters can influence tubulin polymerisation and tubulin depolymerisation.

    摘要翻译: 通式婆罗洲莱斯特(I)其中,R <1>(O)-CH(OR <6>)TC - CH(NR <7A> - [R <7B>) - R的<8>,C(O)-CH( 或<6>) - CH [NR <7>(C(O)-CH(OR <6B>) - CH(NR <7A> - [R <7B>) - R的<8A>)] - R的<8B> [R <7A>,R <7B>是相同的或不同的并且R <7>,R <7>是氢,A,-C(O)R <12>,-C(O)OR <12>,-C (O)SR <12>,-C(O)NHR <9D>,-C(O)NR <9D> - [R <9E>,-SO 2 R <12>,C1-C10烷基,R <8A>,R <8B>是相同的或不同的并且R <8>,R <8>(ⅰ)<3>取代的杂芳基,C7-C16芳烷基,烷基,A B- [O-(CH 2)TC(通过×○ )] 0或1,法尼基 - P(O)(OR <9D>) - O-(CH 2)TC(O) - ,蛋白激酶B抑制剂或法尼基蛋白转移酶的抑制剂,例如 表示法呢,(ii)中,T是一个键,Z的或基团(III),能够将影响微管蛋白聚合的微管蛋白或具有解聚。

    IMMOBILIZABLE RUTHENIUM(II)-CATALYSTS WITH A SUBSTITUTED CENTRAL ATOM, METHOD FOR THE PRODUCTION AND USE THEREOF
    4.
    发明申请
    IMMOBILIZABLE RUTHENIUM(II)-CATALYSTS WITH A SUBSTITUTED CENTRAL ATOM, METHOD FOR THE PRODUCTION AND USE THEREOF 审中-公开
    在中环原子取代,可固定钌(II)催化剂,方法使用和

    公开(公告)号:WO2006018161A3

    公开(公告)日:2006-07-13

    申请号:PCT/EP2005008526

    申请日:2005-08-05

    摘要: The invention relates to immobilizable ruthenium(II)-catalysts having general formulae (I) and (II), containing an SiR' n (OR') 3-n structural group on at least one of the two anions. The invention also relates to a method for the production and use of compounds in a method for the production of ruthenium (II)-catalysts having general formulae (I) and (II) immobilized on inorganic oxide carriers. The invention further relates to the use of compounds having general formulae (I), (la), (II) and (IIa) as catalysts in organic and metalorganic synthesis. Said compounds can be used as catalysts in C-C coupling reactions, hydrogenations, isomerizations, silylations and hydroformylations. They can be used in particular as catalysts in olefin metathetical reactions such as cross metathesis (CM), ring closure metathesis (RCM), ring opening metathesis (ROM), ring opening metathesis-polymerization (ROMP), acyclic diene metathesis-polymerization (ADMET) and En-In metathesis or in a combination of various metathetical reactions.

    摘要翻译: 本发明涉及一种可固定钌(II)通式(I)和(II)的SIR '名词(OR') 3-n的组轴承在催化剂 两个阴离子中的至少一个。 本发明还涉及用于它们的制备方法和在方法中的用途的化合物的用于生产无机氧化物载体固定化的钌(II)通式(Ia)和催化剂(IIa)中。 本发明还提供了通式(I),(IA),(II)和化合物(IIA),如有机和有机金属合成催化剂。 它们可以被用来作为在C-C偶联反应,氢化,异构化,Silylations和加氢甲酰化催化剂。 特别是,它们用作在烯烃复分解反应,如交叉复分解(CM),闭环复分解(RCM),开环复分解(ROM),开环易位聚合(ROMP),无环二烯烃易位聚合(ADMET),催化剂和烯炔结合复分解或不同类型 复分解反应。

    NOVEL BORNEOLS, PROCESSES FOR PRODUCING THEM AND PHARMACEUTICAL USE THEREOF
    6.
    发明申请
    NOVEL BORNEOLS, PROCESSES FOR PRODUCING THEM AND PHARMACEUTICAL USE THEREOF 审中-公开
    新冰片,PROCESS FOR THEIR和制药用

    公开(公告)号:WO1997035839A1

    公开(公告)日:1997-10-02

    申请号:PCT/EP1996001324

    申请日:1996-03-27

    IPC分类号: C07C271/02

    摘要: The disclosure relates to borneol derivatives of general formula (I) wherein: R represents a phenyl residue optionally substituted by halogen atoms, C1-C4 alkyl groups, C1-C4 alkoxy groups, C1-C6 alkoxycarbonyl groups or C1-C8 acyloxy groups; R stands for a hydrogen atom, a C1-C4 alkyl group, substituted aryl, a C1-C6 alkoxycarbonyl group or a C1-C8 acyl group; R stands for a hydrogen atom, a C1-C4 alkyl group, a C1-C4 acyl group or a tri-C1-C4 alkylsilyl group; R and R represent a hydrogen atom, a C1-C4 alkyl residue or a phenyl residue optionally substituted by halogen atoms, C1-C4 alkyl group, C1-C9 alkoxy groups, C1-C4 alkoxycarbonyl groups or C1-C8 acyloxy groups; R and R stand for a hydrogen atom, hydroxy group or a C1-C8 acyloxy group, or together represent a carbon-carbon bond or oxygen atom; or R and R and/or R and R respectively stand together for a carbonyl group, a C1-C4 alkylidene group or if required an oxirane group substituted by a C1-C3 alkyl group. Also disclosed are the salts of these derivatives with physiologically tolerable acids, their alpha -, beta - or gamma -cyclodextrin clathrates and compounds of general formula (I) encapsulated in liposomes.

    摘要翻译: Borneolderivate通式(I)中有所描述,其中R <1>表示任选被卤原子,C1-C4烷基,C1-C4烷氧基,C1-C6烷氧羰基或C 1 -C 8 - 酰氧基苯基取代; [R <2>表示一个氢原子,一个C1-C4烷基,取代的芳基,一个C1-C6烷氧基羰基或C1-C8酰基基团; [R <3>代表氢原子,C1-C4烷基,C1-C4酰基或三C1-C4烷基甲硅烷基,并且其中; [R <4>和R <7>代表氢原子,C1-C4烷基或任选地被卤素原子,C1-C4烷基,C1-C9烷氧基,C1-C4烷氧羰基或C 1 -C 8 - 酰氧基苯基取代的 且R <5>和R <6>代表氢原子,羟基或C1-C8-酰氧基或一起代表碳 - 碳键或氧原子,或R <4>和R <5>和/或R <6> 且R <7>的每个一起表示羰基,C1-C4亚烷基,或者,如果需要的话,由一个C1-C3烷基取代的环氧乙烷基团,和任选地它们的盐与生理上可接受的酸,以及它们的α - ,β - 或伽马-Cyclodextrinclathrate和 通式(I)的脂质体包裹的化合物的意思。

    BORNEOL DERIVATIVES AFFECTING TUBULIN POLYMERIZATION AND DEPOLYMERIZATION
    7.
    发明申请
    BORNEOL DERIVATIVES AFFECTING TUBULIN POLYMERIZATION AND DEPOLYMERIZATION 审中-公开
    微管蛋白聚合或 -DEPOLYMERISATION - 影响BORNEOLDERIVATE

    公开(公告)号:WO1995030650A1

    公开(公告)日:1995-11-16

    申请号:PCT/EP1995001341

    申请日:1995-04-13

    IPC分类号: C07C271/22

    摘要: The invention relates to borneol derivatives of the general formula (I) in which R is C(O)-CH(OR )-CH(NHR )-R , R is hydrogen, -OH, C1-C10-Alkyl, C1-C10-alkoxy, -OC(O)R , -OP(O)(OH)2 or R and R are together an oxygen atom, R is hydrogen, C1-C10-alkyl, -(CH2)n-OR , R is hydrogen, C1-C10-alkyl, -(CH2)p-OR , or R and R together are an oxygen atom, a =CHR group, n is 0 to 8, p is 1 to 8, R is -C(O)R , -SO2R , -C(O)NHR , -C(O)NR R , (formula), R is aryl, R and R are the same or different and represent C1-C10-akyl, C4-C8-cycloalkyl, aryl, C7-C16-aralkyl, R is hydrogen, C1-C10-alkyl, -(CH2)s-OR , s is 1 to 8, R , R and R are the same or different and represent hydrogen, C1-C10-alkyl, aryl, C7-C16 aralkyl, SO2R , -P(O)(OH)2, R and R are the same or different and represent hydrogen, C1-C10-alkyl, aryl, C7-C16-aralkyl, X and X are the same or different and mean X, X may be hydrogen, halogen, -OH, -NO2, -N3, -CN, -NR R , -NHSO2R , -CO2R , C1-C10-alkyl, C1-C10-alkoxy, C1-C10-acyloxy, C1-C10-acyl and, if R is hydrogen, their salts with physiologically tolerable bases, and alpha -, beta - or gamma -cyclodextrin clathrates, and the compounds of the general formula (I) encapsulated with liposomes.

    摘要翻译: 本发明涉及Borneolderivate通式(I)其中R <1> C(O)-CH(OR <6>) - CH(NHR <7>) - R的<8>,R <2>是氢,-OH ,C1-C10烷基,C1-C10烷氧基,-OC(O)R <9A>,-OSO 2 R <9A>,-OP(O)(OH)2,NHR <9>,NR <9> - [R < 图9b>,R <3>是氢,-OH,C1-C10烷氧基,-OC(O)R <9B>,-OSO 2 R <9B>,-OP(O)(OH)2,或R <2>, [R <3>一起为氧原子,R <4>为氢,C1-C10烷基, - (CH 2)N-OR <11A>,R <5>是氢,C1-C10烷基, - (CH 2)p OR <11B>或R <4>,R <5>在一起的氧原子,= CHR <10>基团,n是0至8,p为1至8,R <7> -C(O)R <12? ,-SO> 2 ,-C(O)OR <12>,-C(O)NHR <9D>,-C(O)NR <9D> - [R <9E>中,(a)中,R <8>芳基,R <9A-E>,R <12>是相同的或不同的并且是C 1 -C 10烷基,C 4 -C 8 - 环烷基,芳基,C7-C16芳烷基,R <10>为氢,C 1 -C C10烷基, - (CH 2)S-或<14>,S为1〜8,R <6>,R <11A,b>,R <14>是相同的或不同的,是氢,C1-C10烷基,芳基 ,C7-C16芳烷基,-SO 2 R <9C>平均-P(O)(OH)2,R <13>,R <15A,b>是相同的或不同的并且是氢,C1-C10-A lkyl,芳基,C7-C16芳烷基,X <1>中,X <2>是相同的或不同的,X,X是氢,卤素,-OH,-NO 2,-N 3,-CN,-NR <15A> [R <15B>,-NHSO 2 <15>,-CO 2 R <15>,C1-C10烷基,C1-C10烷氧基,C1-C10酰氧基,可以是C1-C10酰基,和,如果R <15>为氢 基,它们与生理上可耐受的碱的盐,以及它们的α - ,β - 或伽马-Cyclodextrinclathrate,并用通式(I)的脂质体包封的化合物的意思。