1,2 DIHYDRO-3-H-DIBENZ(de,h) ISOQUINOLINE 1,3 DIONE AND THEIR USE AS ANTICANCER AGENTS
    131.
    发明申请
    1,2 DIHYDRO-3-H-DIBENZ(de,h) ISOQUINOLINE 1,3 DIONE AND THEIR USE AS ANTICANCER AGENTS 审中-公开
    1,2二氢-3H-DIBENZ(de,h)异喹啉1,3二酮及其作为反应剂的用途

    公开(公告)号:WO1994006771A1

    公开(公告)日:1994-03-31

    申请号:PCT/US1993008640

    申请日:1993-09-13

    CPC classification number: C07D401/04 C07D221/18 C07D401/06

    Abstract: This invention relates to a compound useful for the treatment of tumors having formula (I), wherein R8, R6 and R10 are independently hydrogen, lower alkyl, aryl, lower alkanoyl, formyl, halogen, hydrazino, nitro, NR2R3, OR1, or SR1, methoxy, hydroxy, CO2H, SO2NR1R2, or CONR1R2; R1, R2 and R3 are independently hydrogen, lower alkyl, aryl lower alkyl, aryl, formyl or lower alkanoyl; R9, R11, R10 and R7 are independently hydrogen, or lower alkyl or R9 and R11 taken together with the carbon atoms to which they are attached form a phenyl group or R9 and R10 taken together with the carbon atoms to which they are attached form a phenyl group or R7 and R10 taken together with the carbon atoms to which they are attached form a phenyl group; A is (CR4R5)n3, lower cycloalkyl or aryl or a chemical bond; each R4 and R5 are independently hydrogen or lower alkyl; R12 and R13 are independently hydrogen, or lower alkyl which is unsubstituted or substituted with hydroxy, mercapto, lower alkoxy, lower alkylcarbonyloxy, carboxy, or carbloweralkoxy or R12 and R13 taken together with the nitrogen to which they are attached form a 3-6-membered heterocyclic ring; D is a chemical bond or taken together with NR12 forms a 5 or 6-membered heterocyclic ring; n1 and n2 are independently 0, 1 or 2; and n3 is 0, 1, 2, 3, 4 or 5.

    Abstract translation: 本发明涉及可用于治疗具有式(I)的肿瘤的化合物,其中R 8,R 6和R 10独立地为氢,低级烷基,芳基,低级烷酰基,甲酰基,卤素,肼基,硝基,NR 2 R 3,OR 1或SR 1 ,甲氧基,羟基,CO2H,SO2NR1R2或CONR1R2; R1,R2和R3独立地是氢,低级烷基,芳基低级烷基,芳基,甲酰基或低级烷酰基; R9,R11,R10和R7独立地为氢,或低级烷基或R9和R11与它们所连接的碳原子一起形成苯基或R 9和R 10与它们所连接的碳原子一起形成 苯基或R 7和R 10与它们所连接的碳原子一起形成苯基; A是(CR4R5)n3,低级环烷基或芳基或化学键; 每个R 4和R 5独立地是氢或低级烷基; R 12和R 13独立地为氢,或未被取代或被羟基,巯基,低级烷氧基,低级烷基羰基氧基,羧基或碳氟烷基氧基取代的低级烷基,或者与它们所连接的氮一起形成的R 12和R 13一起形成3-6元环, 元环杂环; D是化学键或与NR12一起形成5或6元杂环; n1和n2独立地为0,1或2; n3为0,1,2,3,4或5。

    PHOTOCONDUCTIVE POLYMERS
    132.
    发明申请
    PHOTOCONDUCTIVE POLYMERS 审中-公开
    光电聚合物

    公开(公告)号:WO1994004592A1

    公开(公告)日:1994-03-03

    申请号:PCT/US1993007747

    申请日:1993-08-17

    CPC classification number: C08G61/122

    Abstract: The invention relates to polymers which exhibit excellent electronic, optical and mechanical properties. The invention more particularly relates to polymers of the polyquinoline and polyanthrazoline class which are useful in electronic, optoelectronic and photonic applications. The invention further relates to a method of solubilizing polymers of the invention and polyquinolines and polyanthrazolines in general, using a complexing agent of a Lewis acid, a dialkyl phosphate, a diaryl phosphate or mixtures thereof.

    Abstract translation: 本发明涉及具有优异的电子,光学和机械性能的聚合物。 本发明更具体地涉及可用于电子,光电子和光子应用的聚喹啉和聚吡唑啉类的聚合物。 本发明进一步涉及使用路易斯酸,磷酸二烷基酯,磷酸二芳基酯或其混合物的络合剂,增溶本发明的聚合物和聚喹啉和聚吡唑啉的方法。

    RECOGNITION AND SEPARATION OF CARBON CLUSTERS
    134.
    发明申请
    RECOGNITION AND SEPARATION OF CARBON CLUSTERS 审中-公开
    碳聚集体的识别和分离

    公开(公告)号:WO1993022272A1

    公开(公告)日:1993-11-11

    申请号:PCT/US1993003599

    申请日:1993-04-15

    Abstract: Carbon clusters, such as C60 and C70 fullerenes are separated by means of a recognition selector having formula (I), wherein R1 is (a), wherein R2 is O, S or NR12 wherein R12 is independently hydrogen or P=O with the proviso that when R12 is P=O, then only one such group is present and all R2's are additionally bonded to R12, R4 is independently O, S or NH, R3 and R5 are each independently hydrogen or lower alkyl, n and o are each independently zero, 1, 2, or 3, p, q, r, s and t are each independently zero or 1, Ar is a monocyclic or ortho-fused polycyclic aromatic moiety having up to 10 carbon atoms, either of which may be unsubstituted or substituted with one or more lower alkyl, NO2, N(R6)3 , CN, COOR7, SO3H, COR8 and OR9 wherein R6, R7, R8 and R9 are each independently hydrogen or lower alkyl; W is H or CH=CH2; and m is 1 to 10.

    Abstract translation: 通过具有式(I)的识别选择剂分离碳簇,例如C60和C70富勒烯,其中R 1是(a),其中R 2是O,S或NR 12,其中R 12独立地是氢或P = O,条件是 当R 12为P = O时,则仅存在一个这样的基团,并且所有的R 2另外与R 12连接,R 4独立地为O,S或NH,R 3和R 5各自独立地为氢或低级烷基,n和o各自独立地为 0,1,2或3,p,q,r,s和t各自独立地为0或1,Ar是具有至多10个碳原子的单环或邻 - 稠合多环芳族部分,其中任一个可以是未取代的或 被一个或多个低级烷基,NO 2,N(R 6)3+,CN,COOR 7,SO 3 H,COR 8和OR 9取代,其中R 6,R 7,R 8和R 9各自独立地为氢或低级烷基; W是H或CH = CH 2; m为1〜10。

    NOVEL ACYLATED PHOSPHOLIPID DRUGS
    135.
    发明申请
    NOVEL ACYLATED PHOSPHOLIPID DRUGS 审中-公开
    新型聚合磷酸药物

    公开(公告)号:WO1993021191A1

    公开(公告)日:1993-10-28

    申请号:PCT/US1993003650

    申请日:1993-04-16

    CPC classification number: C07F9/10 C07F9/117

    Abstract: The invention relates to a compound having formula (A) or pharmaceutically acceptable salts thereof, wherein one of R1 and R2 is a heteroatom fatty acid acyl group having 13-14 carbon atoms in the principal chain and up to a total of 18 carbon atoms, while the other is hydrogen, a heteroatom of fatty acid acyl group containing 13-14 carbon atoms in the principal chain and up to a total of 18 carbon atoms or an acyl group of a fatty acid containing 4-26 carbon atoms in the principal chain and up to a total of 30 carbon atoms and R is a naturally occurring polar group characteristic of a glycerolphospholipid isolated from endogenous sources. This invention also relates to the use of the compounds of the present invention for inhibiting retrovirus infections and for the treatment of AIDS or AIDS related diseases.

    Abstract translation: 本发明涉及具有式(A)的化合物或其药学上可接受的盐,其中R1和R2之一是在主链中具有13-14个碳原子并且总共18个碳原子的杂原子脂肪酸酰基, 而另一个是氢,在主链中含有13-14个碳原子并且总共18个碳原子的脂肪酸酰基的杂原子或在主链中含有4-26个碳原子的脂肪酸的酰基 和总共30个碳原子,R是从内源分离的甘油磷脂特征的天然存在的极性基团。 本发明还涉及本发明化合物用于抑制逆转录病毒感染和用于治疗AIDS或AIDS相关疾病的用途。

    CHIRAL CATALYSTS, CATALYTIC OXIDATION AND DISPROPORTIONATION REACTIONS, AND METHODS OF PRODUCING EPOXYCHROMANS AND TAXOL
    136.
    发明申请
    CHIRAL CATALYSTS, CATALYTIC OXIDATION AND DISPROPORTIONATION REACTIONS, AND METHODS OF PRODUCING EPOXYCHROMANS AND TAXOL 审中-公开
    CHIRAL CATALYSTS,催化氧化和分解反应,以及生产环氧氯丙烷和紫杉醇的方法

    公开(公告)号:WO1993003838A1

    公开(公告)日:1993-03-04

    申请号:PCT/US1992007261

    申请日:1992-08-26

    Abstract: Chiral catalysts for enantioselectively epoxidizing a prochiral olefin and for enantioselectively oxidizing a prochiral sulfide are disclosed, together with methods of using such catalysts. In accordance with one aspect of the invention, the catalyst is a salen derivative which has general structure (I). In accordance with another aspect of the present invention is a method of producing an epoxychroman using a chiral catalyst. In accordance with this method, a chromene derivative, an oxygen atom source, and a chiral catalyst are reacted under such conditions and for such time as is needed to epoxidize said chromene derivative. In accordance with yet another aspect of this invention is a method of enantioselectively epoxidizing a cis-cinnamate derivative to make taxol or an analog thereof. In accordance with another aspect a method of disproportionation of hydrogen peroxide using the catalysts of the present invention is disclosed.

    Abstract translation: 公开了用于对前向手性环氧化前手性烯烃和对映选择性氧化前手性硫化物的手性催化剂,以及使用这种催化剂的方法。 根据本发明的一个方面,催化剂是具有一般结构(I)的salen衍生物。 根据本发明的另一方面,使用手性催化剂制备环氧苯并二氢吡喃的方法。 根据该方法,在这样的条件下和色素衍生物环氧化所需的时间之间使色烯衍生物,氧原子源和手性催化剂反应。 根据本发明的另一方面是一种对映选择性环氧化顺式肉桂酸衍生物以制备紫杉醇或其类似物的方法。 根据另一方面,公开了使用本发明的催化剂歧化过氧化氢的方法。

    INHIBITION OF CELL PROLIFERATION BY HYDROPHOBIC PEPTIDES
    139.
    发明申请
    INHIBITION OF CELL PROLIFERATION BY HYDROPHOBIC PEPTIDES 审中-公开
    通过疏水肽抑制细胞增殖

    公开(公告)号:WO1992013549A1

    公开(公告)日:1992-08-20

    申请号:PCT/US1992000905

    申请日:1992-02-04

    CPC classification number: C07K5/06043 A61K38/00

    Abstract: The present invention is directed a method of using certain hydrophobic peptides for the inhibition of cell proliferation, wherein the peptides have the general formula: R-Xaa1-(Xaa)m-Xaac. The subject peptides have 2-7 amino acids such as alanine (Ala), arginine (Arg), cysteine (Cys), isoleucine (Ile), leucine (Leu), lysine (Lys), methionine (Met), norleucine (nLeu), phenylalanine (Phe), proline (Pro), threonine (Thr), tyrosine (Tyr), tryptophan (Trp), or valine (Val). In accordance with the present invention, these peptides are potent inhibitors of cell proliferation as well as inhibitors of the synthesis of two cellular proto-oncogenes. One aspect of the present invention provides for the prevention and treatment of cancer by administration of the subject peptides. A further aspect of the present invention provides for inhibiting cell proliferation using the subject peptides in the treatment and prevention of prostatic hypertrophy, arterial occlusion (restenosis), arteriosclerosis, and smooth muscle cell diseases.

    Abstract translation: 本发明涉及一种使用某些疏水肽抑制细胞增殖的方法,其中肽具有以下通式:R-Xaa1-(Xaa)m-Xaac。 主题肽具有丙氨酸(Ala),精氨酸(Arg),半胱氨酸(Cys),异亮氨酸(Ile),亮氨酸(Leu),赖氨酸(Lys),甲硫氨酸(Met),正亮氨酸(nLeu) ,苯丙氨酸(Phe),脯氨酸(Pro),苏氨酸(Thr),酪氨酸(Tyr),色氨酸(Trp)或缬氨酸(Val)。 根据本发明,这些肽是细胞增殖的有效抑制剂以及合成两种细胞原癌基因的抑制剂。 本发明的一个方面提供了通过施用本发明肽来预防和治疗癌症。 本发明的另一方面提供了使用本发明肽在治疗和预防前列腺肥大,动脉闭塞(再狭窄),动脉硬化和平滑肌细胞疾病中抑制细胞增殖。

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