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1. 发明专利

IL263504D0 Nanoemulsion compositions of taxoid drugs, and methods for the use thereof to target cancer cells and cancer stem cells 未知
公开(公告)号：IL263504D0
公开(公告)日：2019-01-31
申请号：IL26350418
申请日：2018-12-04
申请人： TARGAGENIX INC , UNIV NEW YORK STATE RES FOUND , UNIV NORTHEASTERN , JAMES E EGAN , IWAO OJIMA , MANSOOR M AMIJI , GALINA IVANOVNA BOTCHKINA
发明人： JAMES E EGAN , IWAO OJIMA , MANSOOR M AMIJI , GALINA IVANOVNA BOTCHKINA
IPC分类号： A61K20060101
摘要： A composition of an omega-3 polyunsaturated fatty acid (PUFA)-taxoid conjugate encapsulated in an oil-in-water nanoemulsion (NE) drug delivery system. A method of treating cancer by administering an effective amount of a pharmaceutical composition including a PUFA-taxoid conjugate encapsulated in an oil-in-water NE drug delivery system to a subject in need of treatment, and treating cancer. A method of overcoming multidrug resistance by exposing a multidrug resistant cell to an effective amount of a pharmaceutical composition including an omega-3 polyunsaturated fatty acid (PUFA)-taxoid conjugate encapsulated in an oil-in-water NE drug delivery system, and inducing the death of the multidrug resistant cell. A method of eliminating a cancer stem cell. Methods of reducing stemness of a cancer stem cell, retaining drug in the body, and providing a slower release profile.

2. 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:

3. 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:

4. 发明申请

US20100021471A1 CARBON NANOTUBE-BASED DRUG DELIVERY SYSTEMS AND METHODS OF MAKING SAME 审中-公开
标题翻译：基于碳纳米管的药物输送系统及其制备方法
公开(公告)号：US20100021471A1
公开(公告)日：2010-01-28
申请号：US12179887
申请日：2008-07-25
申请人： Jingyi Chen , Stanislaus S. Wong , Iwao Ojima
发明人： Jingyi Chen , Stanislaus S. Wong , Iwao Ojima
IPC分类号： A61K39/395 , A61K31/415 , A61K31/495 , A61K31/715 , A61K31/337 , A61P35/00
CPC分类号： A61K31/337 , A61K9/0019 , A61K47/557 , A61K47/6929 , B82Y5/00
摘要： The present invention includes a conjugates comprising a carbon nanotube with at least one covalently attached recognition module, and at least one covalently attached pharmaceutical compound or a precursor of the pharmaceutical compound,wherein the pharmaceutical compound, or precursor of the pharmaceutical compound, is attached to the carbon nanotube by a linker moiety.
摘要翻译：本发明包括具有至少一个共价连接的识别模块的碳纳米管和至少一种共价连接的药物化合物或药物化合物的前体的缀合物，其中该药物化合物或该药物化合物的前体附着于碳纳米管通过接头部分。

5. 发明授权

US07615653B2 Anti-tuberculosis taxane compounds 有权
标题翻译：抗结核紫杉烷化合物
公开(公告)号：US07615653B2
公开(公告)日：2009-11-10
申请号：US11684883
申请日：2007-03-12
申请人： Iwao Ojima
发明人： Iwao Ojima
IPC分类号： C07D305/00
CPC分类号： C07D305/14
摘要： The present invention relates to compounds having the formula (I):
摘要翻译：本发明涉及具有式（I）的化合物：

6. 发明申请

US20080081836A1 Anti-Tuberculosis Taxane Compounds 有权
标题翻译：抗结核紫杉烷化合物
公开(公告)号：US20080081836A1
公开(公告)日：2008-04-03
申请号：US11684883
申请日：2007-03-12
申请人： Iwao Ojima
发明人： Iwao Ojima
IPC分类号： A61K31/337 , C07D305/02
CPC分类号： C07D305/14
摘要： The present invention relates to compounds having the formula (I):
摘要翻译：本发明涉及具有式（I）的化合物：

7. 发明授权

US6096909A 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：US6096909A
公开(公告)日：2000-08-01
申请号：US910742
申请日：1997-08-13
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： C07F7/1856 , C07D305/14 , Y02P20/55
摘要： This invention relates to a taxoid of the formula (I) ##STR1## wherein R.sup.1 is 1-propenyl 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 represents a hydrogen or a hydroxyl protecting group;R.sup.6 represents an acyl radical,which are useful as antitumor agents or their precursors. A pharmaceutical composition having antineoplastic activity comprising the compound of formula (I) and a physiologically acceptable carrier and method of treatment are also disclosed.
摘要翻译：本发明涉及式（I）的紫杉烷，其中R 1是1-丙烯基; 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表示氢或羟基保护基; R6表示酰基，其可用作抗肿瘤剂或其前体。还公开了包含式（I）化合物和生理学上可接受的载体和治疗方法的具有抗肿瘤活性的药物组合物。

8. 发明授权

US5705508A Anti-tumor compounds, pharmaceutical compositions, methods for preparation thereof and for treatment 失效
标题翻译：抗肿瘤化合物，药物组合物，其制备方法和治疗方法
公开(公告)号：US5705508A
公开(公告)日：1998-01-06
申请号：US542537
申请日：1995-10-13
申请人： Iwao Ojima , Ezio Bombardelli
发明人： Iwao Ojima , Ezio Bombardelli
IPC分类号： A61K31/00 , A61K31/335 , A61K31/337 , A61P35/00 , C07D205/08 , C07D305/14 , C07F7/18 , A61K31/445 , C07D305/00
CPC分类号： C07D305/14 , C07D205/08 , C07F7/186 , Y02P20/55
摘要： The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## with .beta.-lactams of formula (V). ##STR2## The invention also provides pharmaceutical compositions including the novel taxanes and methods for treatment of certain cancers with these new compounds.
摘要翻译：本发明涉及可用作化学治疗剂或其前体的新型紫杉烷。用于制备新型紫杉烷的方法包括在碱存在下式（III）或（IV）的葡萄糖抑制剂（V）的偶联反应。（V）本发明还提供药物组合物，其包括新型紫杉烷类和用这些新化合物治疗某些癌症的方法。

9. 发明授权

US5599820A Anti-tumor compounds, pharmaceutical compositions, methods for preparation thereof and for treatment 失效
标题翻译：抗肿瘤化合物，药物组合物，其制备方法和治疗方法
公开(公告)号：US5599820A
公开(公告)日：1997-02-04
申请号：US461730
申请日：1995-06-05
申请人： Iwao Ojima , Ezio Bombardelli
发明人： Iwao Ojima , Ezio Bombardelli
IPC分类号： A61K31/00 , A61K31/335 , A61K31/337 , A61P35/00 , C07D205/08 , C07D305/14 , C07F7/18 , A61K31/445 , A61K31/21
CPC分类号： C07D305/14 , C07D205/08 , C07F7/186 , Y02P20/55
摘要： The present invention is directed to novel taxanes useful as chemotherapeutic agents or their precursors. Processes for preparing the novel taxanes include coupling reactions, in the presence of a base, of baccatin of formula (III) or (IV) ##STR1## with .beta.-lactams of formula (V). ##STR2## The invention also provides pharmaceutical compositions including the novel taxanes and methods for treatment of certain cancers with these new compounds.
摘要翻译：本发明涉及可用作化学治疗剂或其前体的新型紫杉烷。用于制备新型紫杉烷的方法包括在碱存在下式（III）或（IV）的葡萄糖抑制剂（V）的偶联反应。（V）本发明还提供药物组合物，其包括新型紫杉烷类和用这些新化合物治疗某些癌症的方法。

10. 发明授权

US5338725A Anti-aggregatory agents for platelets 失效
公开(公告)号：US5338725A
公开(公告)日：1994-08-16
申请号：US906525
申请日：1992-06-30
申请人： Iwao Ojima , Masakatsu Eguchi , Young-Im Oh , Barry S. Coller
发明人： Iwao Ojima , Masakatsu Eguchi , Young-Im Oh , Barry S. Coller
IPC分类号： A61K38/00 , C07K7/02 , C07K14/75 , A61K37/02 , C07K7/06 , C07K7/08
CPC分类号： C07K14/75 , C07K7/02 , A61K38/00
摘要： The present invention provides synthetic antiaggregatory agents for preventing inhibition of fibrinogen-platelet binding. These anti-aggregatory agents have the general formulas (1)-(5).H--[--(AA.sub.i).sub.i --R--G--D--(AA.sub.j).sub.j --].sub.n --Cx (1)[Ri--C(O)--R--G--D--(AA.sub.j).sub.j --].sub.n --CX (2)Cy--[--AA.sub.i).sub.i --R--G--D--(AA.sub.j).sub.i --].sub.n --Z (3)H--[--(AA.sub.i).sub.i --R--G--D--(AA.sub.j).sub.j --].sub.n --CZ--[--(AA.sub.k).sub.k --R--G--D--(AA.sub.l).sub.l --].sub.m --Z (4)[R.sub.1 --C(O)--R--G--D--(AA.sub.i).sub.i --].sub.n --CZ[--(AA.sub.j).sub.j ]--R--G--D--(AA.sub.k).sub.k --].sub.m --Z (5)in which: R=Arg; G=Gly; D=Asp; AA.sub.i, AA.sub.j, AA.sub.k and AA.sub.l = alpha-, beta- and omega-amino acid residues; (AA.sub.i).sub.i (AA.sub.j).sub.j =peptide chains having the same or different amino acid residues; (AA.sub.k).sub.k =peptide chains having the same or different amino acid residues; (AA.sub.l).sub.l =peptide chains having the same or different amino acid residues; i and j =integers 0-20; m =an integer 1-10; n=an integer 2-10; Cx =a conjugator bearing at least two amine residues in a molecule having 1-30 carbon atoms, i.e, diamines, triamines, tetramines, and polyamines, which can have other functional groups in the molecule; Cy =a conjugator bearing at least two carboxyl residues in a molecule having 1-30 carbon atoms, i.e., aliphatic, aromatic, heteroaromatic, cycloalkyl dicarboxylic acid, tricarboxylic acid, and polycarboxylic acid residues, which can have other functional groups in the molecule; Cz .sup.= a conjugator bearing at least one amine residue and one carboxyl residue in an aromatic or a cycloalkyl skeleton, having 1-30 carbon atoms, i.e., aromatic, heteroaromatic and cycloalkyl amino carboxylic acid, diamino carboxylic acid, diamino dicarboxylic acid, and ployamino polycarboxylic acid residues; R.sub.1 =an alkyl, aromatic, heteroaromatic, or cycloalkyl group having 1-30 carbons, which can have other functional groups in the molecule; and Z=carboxyl, amide, N-substituted amide, hydrazide, N-substituted hydrazide, or ester group.

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