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1. 发明申请

US20150183715A1 ALPHA- AND GAMMA-TRUXILLIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF 有权
标题翻译： ALPHA和GAMMA-TRUXILLIC酸衍生物及其药物组合物
公开(公告)号：US20150183715A1
公开(公告)日：2015-07-02
申请号：US14413621
申请日：2013-07-19
申请人： Iwao Ojima , Dale Deutsch , Martin Kaczocha , William T. Berger , Robert Rizzo , Trent E. Balius
发明人： Iwao Ojima , Dale Deutsch , Martin Kaczocha , William T. Berger , Robert Rizzo , Trent E. Balius
IPC分类号： C07C69/757 , C07C67/48 , G01N33/566 , C07C67/08
CPC分类号： A61K31/216 , A61K31/194 , C07B2200/07 , C07C67/08 , C07C67/48 , C07C69/753 , C07C69/757 , C07C69/76 , C07C211/58 , C07C233/11 , C07C233/58 , C07C235/38 , C07C235/40 , C07C2601/04 , G01N33/566 , G01N33/68 , G01N2333/47 , G01N2500/04 , G01N2500/20
摘要： The present invention provides a compound, and method of inhibiting the activity of a Fatty Acid Binding Protein (FABP) comprising contacting the FABP with a compound, having the structure:
摘要翻译：本发明提供一种化合物和抑制脂肪酸结合蛋白（FABP）活性的方法，包括使FABP与化合物接触，所述化合物具有以下结构：

2. 发明授权

US07981926B2 Fluorotaxoids 有权
标题翻译：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。

3. 发明授权

US07847119B2 Drug conjugates 有权
标题翻译：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。

4. 发明申请

US20080139815A1 DRUG CONJUGATES 有权
标题翻译：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。

5. 发明授权

US06593482B2 Methods for preparing new taxoids and pharmaceutical compositions containing them 失效
标题翻译：制备新紫杉烷和含有它们的药物组合物的方法
公开(公告)号：US06593482B2
公开(公告)日：2003-07-15
申请号：US10029954
申请日：2001-12-31
申请人： Hervé Bouchard , Jean-Dominique Bourzat , Alain Commerçon , Iwao Ojima
发明人： Hervé Bouchard , Jean-Dominique Bourzat , Alain Commerçon , Iwao Ojima
IPC分类号： C07D30500
CPC分类号： C07D205/08 , C07D305/14
摘要： Methods of preparing methylthiomethyloxy taxoids of formula (XXXIV) from baccatin and &bgr;-lactam are presented. These new taxoids display noteworthy anti-tumor and anti-leukemic properties.
摘要翻译：提出了从浆果赤霉素和β-内酰胺制备式（XXXIV）的甲硫基甲氧基紫杉烷的方法。这些新型紫杉醇具有显着的抗肿瘤和抗白血病特性。

6. 发明授权

US6100411A Taxoid anti-tumor agents and pharmaceutical compositions thereof 失效
标题翻译：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。

7. 发明授权

US4581452A Production of 5-perfluoroalkyldihydrouracil derivatives 失效
标题翻译：生产5-全氟烷基二氢尿嘧啶衍生物
公开(公告)号：US4581452A
公开(公告)日：1986-04-08
申请号：US526880
申请日：1983-08-26
申请人： Iwao Ojima , Takamasa Fuchikami , Makoto Fujita
发明人： Iwao Ojima , Takamasa Fuchikami , Makoto Fujita
IPC分类号： A61K31/505 , A61P35/00 , C07C51/10 , C07C51/60 , C07C275/16 , C07C275/24 , C07C275/28 , C07C335/08 , C07C335/12 , C07C335/16 , C07D239/22 , C07H13/12 , C07H19/06 , C07C57/03 , C07C157/05
CPC分类号： C07D239/22 , C07C275/16 , C07C275/24 , C07C275/28 , C07C335/08 , C07C335/12 , C07C335/16 , C07C51/10 , C07C51/60 , C07H13/12 , C07H19/06
摘要： A process for preparing a 5-perfluoroalkyl-dihydrouracil derivative of the general formula ##STR1## wherein R.sub.f represents a perfluoroalkyl group, each of R.sup.1 and R.sup.2 represents a hydrogen atom, or an alkyl, cycloalkyl, aryl, aralkyl or heterocyclic group, and Y is an oxygen or sulfur atom, which comprises (a) reacting a compound of the general formula ##STR2## wherein X represents a halogen atom or hydroxyl group, with a urea derivative of the general formula ##STR3## provided that when X is a hydroxyl group and at least one of R.sup.1 and R.sup.2 is a hydrogen atom, said reaction is carried out in the presence of a condensing agent, or (b) cyclizing a compound of the general formula ##STR4## and a novel intermediate compound of the above formula (IV).
摘要翻译：制备通式（I）的5-全氟烷基 - 二氢尿嘧啶衍生物的方法，其中R f表示全氟烷基，R 1和R 2各自表示氢原子或烷基，环烷基，芳基，芳烷基或杂环基并且Y是氧或硫原子，其包括（a）使其中X表示卤素原子或羟基的通式为“IMAGE”（II）的化合物与通式为“IMAGE”的脲衍生物 III），条件是当X是羟基并且R 1和R 2中的至少一个是氢原子时，所述反应在缩合剂的存在下进行，或（b）使通式为“IMAGE”的化合物环化，（IV）和上述式（IV）的新型中间体化合物。

8. 发明授权

US4352752A Process for the preparation of dipeptides 失效
标题翻译：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。

9. 发明申请

US20170216241A1 ALPHA- AND GAMMA-TRUXILLIC ACID DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF 审中-公开
公开(公告)号：US20170216241A1
公开(公告)日：2017-08-03
申请号：US15429656
申请日：2017-02-10
申请人： Iwao Ojima , Dale Deutsch , Martin Kaczocha , William T. Berger , Robert Rizzo , Trent E. Balius
发明人： Iwao Ojima , Dale Deutsch , Martin Kaczocha , William T. Berger , Robert Rizzo , Trent E. Balius
IPC分类号： A61K31/216 , G01N33/68 , A61K31/194
CPC分类号： A61K31/216 , A61K31/194 , C07B2200/07 , C07C67/08 , C07C67/48 , C07C69/753 , C07C69/757 , C07C69/76 , C07C211/58 , C07C233/11 , C07C233/58 , C07C235/38 , C07C235/40 , C07C2601/04 , G01N33/566 , G01N33/68 , G01N2333/47 , G01N2500/04 , G01N2500/20
摘要： The present invention provides a compound, and method of inhibiting the activity of a Fatty Acid Binding Protein (FABP) comprising contacting the FABP with a compound, having the structure:

10. 发明授权

US09604904B2 Alpha- and gamma-truxillic acid derivatives and pharmaceutical compositions thereof 有权
公开(公告)号：US09604904B2
公开(公告)日：2017-03-28
申请号：US14413621
申请日：2013-07-19
申请人： Iwao Ojima , Dale Deutsch , Martin Kaczocha , William T. Berger , Robert Rizzo , Trent E. Balius
发明人： Iwao Ojima , Dale Deutsch , Martin Kaczocha , William T. Berger , Robert Rizzo , Trent E. Balius
IPC分类号： A61K31/216 , C07C69/757 , C07C67/08 , C07C211/58 , C07C233/11 , C07C233/58 , C07C235/38 , C07C235/40 , C07C69/753 , C07C69/76 , C07C67/48 , G01N33/566
CPC分类号： A61K31/216 , A61K31/194 , C07B2200/07 , C07C67/08 , C07C67/48 , C07C69/753 , C07C69/757 , C07C69/76 , C07C211/58 , C07C233/11 , C07C233/58 , C07C235/38 , C07C235/40 , C07C2601/04 , G01N33/566 , G01N33/68 , G01N2333/47 , G01N2500/04 , G01N2500/20
摘要： The present invention provides a compound, and method of inhibiting the activity of a Fatty Acid Binding Protein (FABP) comprising contacting the FABP with a compound, having the structure:

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