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    Process for production of N-acyl-.alpha.-amino acids
    2.
    发明授权
    Process for production of N-acyl-.alpha.-amino acids 失效
    制备N-酰基-α-氨基酸的方法

    公开(公告)号：US4497964A

    公开(公告)日：1985-02-05

    申请号：US441853

    申请日：1982-11-15

    申请人： Iwao Ojima ,  Kenji Hirai

    发明人： Iwao Ojima ,  Kenji Hirai

    IPC分类号： C07C231/00 ,  B01J31/00 ,  B01J31/12 ,  B01J31/16 ,  B01J31/20 ,  C07C51/12 ,  C07C67/00 ,  C07C231/12 ,  C07C233/47

    CPC分类号： C07C231/12 ,  B01J31/0212 ,  B01J31/20 ,  B01J2231/34 ,  B01J2531/845

    摘要： A process for the production of an N-acyl-.alpha.-amino acid represented by the general formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4, independently from each other, represent a hydrogen atom, an alkyl or cycloalkyl group which may be substituted, or an aryl or heteroaromatic group selected from the group consisting of furyl, pyrrolyl, pyridinyl, thienyl and indolyl which may be substituted, which comprises reacting an oxirane represented by the general formula ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, an amide compound represented by the general formulaR.sup.3 CONHR.sup.4 (III)wherein R.sup.3 and R.sup.4 are as defined above, and carbon monoxide in the presence of hydrogen, a cobalt-containing catalyst, and a promoter composed of a compound containing a metal selected from Groups I, II, III and IV of the periodic table.

    摘要翻译： 由通式（I）表示的N-酰基-α-氨基酸的制备方法，其中R 1，R 2，R 3和R 4彼此独立地表示氢原子，烷基或环烷基 或者可以被取代的芳基或杂芳基，或者可以被取代的呋喃基，吡咯基，吡啶基，噻吩基和吲哚基的芳基或杂芳族基，其中包括使通式（II）表示的环氧乙烷与式 R2如上定义，由通式R 3 CONHR 4（III）表示的酰胺化合物，其中R 3和R 4如上所定义，一氧化碳在氢存在下，含钴催化剂和由含有 选自周期表第I，II，III和IV族的金属。

    Fluorotaxoids
    4.
    发明授权
    Fluorotaxoids 有权
    荧光素类

    公开(公告)号：US07981926B2

    公开(公告)日：2011-07-19

    申请号：US11990323

    申请日：2006-08-11

    申请人： Iwao Ojima

    发明人： Iwao Ojima

    IPC分类号： C07D305/14 ,  A61K31/337

    CPC分类号： C07D305/14

    摘要： The invention relates to fluorinated second generation taxoid compounds, pharmaceutical formulations thereof, and their use for inhibiting the growth of cancer cells in a mammal.

    摘要翻译： 本发明涉及氟化第二代紫杉烷化合物，其药物制剂及其用于抑制哺乳动物癌细胞生长的用途。

    Drug conjugates
    5.
    发明授权
    Drug conjugates 有权
    药物偶联物

    公开(公告)号：US07847119B2

    公开(公告)日：2010-12-07

    申请号：US11856317

    申请日：2007-09-17

    申请人： Iwao Ojima

    发明人： Iwao Ojima

    IPC分类号： C07C321/20

    CPC分类号： C07D305/14 ,  A61K47/6803 ,  A61K47/6889 ,  C07C323/62 ,  C07D213/71

    摘要： A compound having the formula Y-A-Z, wherein: A is a phenyl group which is unsubstituted or substituted; Y and Z are substituents at adjacent positions on ring A; Y represents: Z represents: and wherein the remaining variables are as defined in the specification.

    摘要翻译： 具有式Y-A-Z的化合物，其中：A是未取代或取代的苯基; Y和Z是环A上相邻位置的取代基; Y表示：Z表示：并且其中剩余变量如说明书中所定义。

    DRUG CONJUGATES
    6.
    发明申请
    DRUG CONJUGATES 有权
    药物联合

    公开(公告)号：US20080139815A1

    公开(公告)日：2008-06-12

    申请号：US11856317

    申请日：2007-09-17

    申请人： Iwao Ojima

    发明人： Iwao Ojima

    IPC分类号： C07D213/70 ,  C07C323/62 ,  C07D305/14

    CPC分类号： C07D305/14 ,  A61K47/6803 ,  A61K47/6889 ,  C07C323/62 ,  C07D213/71

    摘要： A compound having the formula Y-A-Z, wherein:A is a 5, 6, or 7 member ring that is monocyclic or is fused to 1 to 3 additional 4 to 8 member rings; wherein ring A and, independently, the fused additional rings are carbocyclic or heterocyclic, and saturated or unsaturated, wherein unsaturated rings are aromatic or non-aromatic; wherein Y and Z are substituents at adjacent positions on ring A;Y represents: Z represents: X and E represent O, S, or NRa or NRb; each of a, b, c, d, e and f independently represents 0 or 1; a+c equals 0, 1, or 2; b+d equals 0, 1, or 2; a+b+c+d+e+f equals 1, 2, or 3; provided that when f is 1, then d is 1, and when d is 0, then f is 0; and when both e and b are 0, then neither R1 nor R2 is chloro or bromo; v represents 0 or 1, provided that when v is 0, then J is hydrogen, a metal ion, or a quaternary ammonium ion, and X is O and G is H;either G is hydrogen, a metal ion, a quaternary ammonium ion, lower alkyl, or comprised of a pharmaceutically active chemical compound or the precursor thereof; or X-G represents a carbonyl-activating group;J is lower alkyl, aryl, heteroaryl, omega-hydroxycarbonyl-(lower alkyl), omega-(lower alkoxy)carbonyl-(lower alkyl), omega-(X-G)-carbonyl-(lower alkyl) group, or comprised of a specific binding agent; and Ra, Rb, R1, R2, R3, R4 are as defined in the specification.

    摘要翻译： 具有式Y-A-Z的化合物，其中：A为5,6或7元环，其为单环或稠合至1至3个另外的4至8个成员环; 其中环A和独立地稠合的另外的环是碳环或杂环的，饱和或不饱和的，其中不饱和环是芳族或非芳族的; 其中Y和Z是环A上相邻位置的取代基; Y表示：Z表示：X和E表示O，S或NR a或NR b。 a，b，c，d，e和f各自独立地表示0或1; a + c等于0,1或2; b + d等于0,1或2; a + b + c + d + e + f等于1,2或3; 条件是当f为1时，d为1，当d为0时，f为0; 当e和b都为0时，R 1和R 2都不是氯或溴; v表示0或1，条件是当v为0时，J为氢，金属离子或季铵离子，X为O且G为H; G是氢，金属离子，季铵离子，低级烷基，或由药物活性化合物或其前体组成; 或X-G表示羰基活化基团; J是低级烷基，芳基，杂芳基，ω-羟基羰基 - （低级烷基），ω-（低级烷氧基）羰基 - （低级烷基），ω-（XG） - 羰基 - （低级烷基） 粘合剂; R 1，R 2，R 1，R 2，R 3，R 3， R 4如本说明书中所定义。

    Taxoid anti-tumor agents and pharmaceutical compositions thereof
    8.
    发明授权
    Taxoid anti-tumor agents and pharmaceutical compositions thereof 失效
    紫杉烷类抗肿瘤剂及其药物组合物

    公开(公告)号：US6100411A

    公开(公告)日：2000-08-08

    申请号：US608003

    申请日：1996-03-04

    申请人： Iwao Ojima

    发明人： Iwao Ojima

    IPC分类号： A61K31/335 ,  A61K31/337 ,  A61P35/00 ,  C07D305/14 ,  C07F7/18

    CPC分类号： C07D305/14 ,  C07F7/1856 ,  Y02P20/55

    摘要： This invention relates to a taxoid of the formula (I): ##STR1## wherein R.sup.1 is a C.sub.3 -C.sub.5 alkyl or alkenyl or trifluoromethyl radical;R.sup.2 is a C.sub.3 -C.sub.5 branched alkyl radical;R.sup.3 and R.sup.4 are independently selected from hydrogen and hydroxyl protecting groups including functional groups which increase the water solubility of the taxoid antitumor agent;R.sup.5 is a hydrogen, an acyl radical, or an alkoxylcarbonyl or carbamoyl radical; andR.sup.6 is an acyl radical.The compounds of formula I are useful as antitumor agents or their precursors. This invention also relates to a pharmaceutical composition having antineoplastic activity comprising the compound of formula (I) and a physiologically acceptable carrier and method of treatment using the compound of formula I.

    摘要翻译： 本发明涉及式（I）的紫杉烷：其中R1是C3-C5烷基或烯基或三氟甲基; R2是C3-C5支链烷基; R3和R4独立地选自氢和羟基保护基，包括增加紫杉烷类抗肿瘤剂的水溶性的官能团; R5是氢，酰基或烷氧基羰基或氨基甲酰基; R6为酰基。 式I的化合物可用作抗肿瘤剂或其前体。 本发明还涉及具有抗肿瘤活性的药物组合物，其包含式（I）化合物和生理学上可接受的载体和使用式I化合物的治疗方法。

    Process for the preparation of dipeptides
    10.
    发明授权
    Process for the preparation of dipeptides 失效
    制备二肽的方法

    公开(公告)号：US4352752A

    公开(公告)日：1982-10-05

    申请号：US240983

    申请日：1981-03-05

    申请人： Iwao Ojima ,  Shigemi Suga

    发明人： Iwao Ojima ,  Shigemi Suga

    IPC分类号： B01J23/00 ,  C07B61/00 ,  C07C67/00 ,  C07C231/00 ,  C07C231/10 ,  C07C235/34 ,  C07C237/12 ,  C07C237/20 ,  C07C237/22 ,  C07D205/08 ,  C07D205/085 ,  C07K1/113 ,  C07K1/12 ,  C07K5/06 ,  C07C103/52 ,  C07C101/30 ,  C07C101/72

    CPC分类号： C07K1/12 ,  C07D205/08 ,  C07D205/085

    摘要： There is provided a novel process for the preparation of a dipeptide represented by the formula: ##STR1## wherein Ar represents an aromatic group; R.sup.1 represents a hydrogen atom, an alkyl group or an aryl group; R.sup.2 represents a hydrogen atom, an alkyl group or an aromatic group; Y represents a hydroxy group, an amino group or an acylamino group, which comprises subjecting a .beta.-lactam compound represented by the formula: ##STR2## wherein Ar, R.sup.1 and R.sup.2 have the same meanings as defined above, and X represents a hydroxy group, an amino group or an acylamino group, an azido group or a benzyloxy group, to hydrogenolysis in the presence of a catalyst. The process can be practiced without any complicated procedure as seen in the conventional processes for the preparation of peptides.

    摘要翻译： 提供了制备由下式表示的二肽的新方法：其中Ar表示芳族基团; R1表示氢原子，烷基或芳基; R2表示氢原子，烷基或芳基; Y表示羟基，氨基或酰氨基，其包括使由下式表示的β-内酰胺化合物：其中Ar，R 1和R 2具有与上述相同的含义，X表示羟基 ，氨基或酰氨基，叠氮基或苄氧基，在催化剂存在下氢解。 该方法可以在没有任何复杂的程序的情况下进行，如在用于制备肽的常规方法中所见。