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1. 发明授权

US09089605B2 Quinone derivatives, pharmaceutical compositions, and uses thereof 有权
标题翻译：醌衍生物，药物组合物及其用途
公开(公告)号：US09089605B2
公开(公告)日：2015-07-28
申请号：US12679828
申请日：2008-09-22
申请人： Mark R. Kelley , Richard F. Borch , Rodney L. Nyland, II
发明人： Mark R. Kelley , Richard F. Borch , Rodney L. Nyland, II
IPC分类号： C07D233/02 , A61K31/196 , A61K45/06 , A61K31/122 , A61K31/13 , A61K31/195 , A61K31/203 , A61K31/282 , A61K31/454
CPC分类号： A61K31/201 , A61K31/122 , A61K31/13 , A61K31/195 , A61K31/198 , A61K31/203 , A61K31/282 , A61K31/454 , A61K31/7068 , A61K33/24 , A61K39/3955 , A61K45/06 , A61K2300/00
摘要： This application describes quinone derivatives which target the redox site of Ape1/Ref1. Also included in the invention are pharmaceutical formulations containing the derivatives and therapeutic uses of the derivatives.
摘要翻译：本申请描述了靶向Ape1 / Ref1的氧化还原位点的醌衍生物。本发明还包括含有衍生物的衍生物和治疗用途的药物制剂。

2. 发明申请

US20100297113A1 QUINONE DERIVATIVES, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF 有权
标题翻译：喹诺酮衍生物，药物组合物及其用途
公开(公告)号：US20100297113A1
公开(公告)日：2010-11-25
申请号：US12679828
申请日：2008-09-22
申请人： Mark R. Kelley , Richard F. Borch , Rodney L. Nyland Ii
发明人： Mark R. Kelley , Richard F. Borch , Rodney L. Nyland Ii
IPC分类号： A61K39/395 , C07C59/90 , C07D233/02 , A61K31/4164 , A61K31/192 , A61P35/00 , A61P11/06 , A61K33/24 , A61K31/454 , A61K31/7068 , A61K31/196
CPC分类号： A61K31/201 , A61K31/122 , A61K31/13 , A61K31/195 , A61K31/198 , A61K31/203 , A61K31/282 , A61K31/454 , A61K31/7068 , A61K33/24 , A61K39/3955 , A61K45/06 , A61K2300/00
摘要： This application describes quinone derivatives which target the redox site of Ape1/Ref1. Also included in the invention are pharmaceutical formulations containing the derivatives and therapeutic uses of the derivatives.
摘要翻译：本申请描述了靶向Ape1 / Ref1的氧化还原位点的醌衍生物。本发明还包括含有衍生物的衍生物和治疗用途的药物制剂。

3. 发明授权

US06903081B2 Phosphoramidates and methods therefor 失效
公开(公告)号：US06903081B2
公开(公告)日：2005-06-07
申请号：US09822376
申请日：2001-03-30
申请人： Richard F. Borch , Hugo Garrido-Hernandez , Sandra C. Tobias
发明人： Richard F. Borch , Hugo Garrido-Hernandez , Sandra C. Tobias
IPC分类号： A61K45/00 , A61K31/165 , A61K31/167 , A61K31/7068 , A61K31/7072 , A61K38/00 , A61P35/00 , A61P43/00 , C07F9/09 , C07F9/24 , C07F9/26 , C07F9/6539 , C07F9/655 , C07F9/6553 , C07H19/10 , A61K31/664
CPC分类号： C07H19/10 , C07F9/2458 , C07F9/26 , C07F9/65515 , C07F9/655345
摘要： Novel phosphoramidate derivatives of hydroxy functional or amino functional compounds, including amino acids, peptides, peptidomimetics and nucleotide analogs, are described. The compounds enable enhanced intracellular delivery of drugs as their corresponding phosphate esters or amides. Described phosphoramidate compounds exhibit antiproliferative activity. Pharmaceutical formulations are provided for treatment of cancers.

4. 发明授权

US5767086A Bone marrow stimulation by certain glutathione analogs 失效
标题翻译：某些谷胱甘肽类似物对骨髓的刺激
公开(公告)号：US5767086A
公开(公告)日：1998-06-16
申请号：US482645
申请日：1995-06-07
申请人： Lawrence M. Kauvar , Matthew H. Lyttle , Amy S. Morgan , Richard F. Borch
发明人： Lawrence M. Kauvar , Matthew H. Lyttle , Amy S. Morgan , Richard F. Borch
IPC分类号： A61K38/00 , A61K38/06 , C07K5/02 , C07K5/037 , G01N30/02 , C07K5/08
CPC分类号： A61K38/06 , C07K5/0215 , G01N30/02
摘要： Compounds of the formula ##STR1## and the esters, amides, amide/esters and salts thereof, wherein YCO is .gamma.-glu or .beta.-asp; G* is phenyl glycine or glycine; Z is CH.sub.2, O or S; and X is a hydrocarbon radical of 1-20 C; are useful in stimulating the differentiation of bone marrow, mitigating the bone-marrow-destructive effects of a chemotherapeutic agent, and in potentiating the toxicity of chemotherapeutic agents.
摘要翻译：式（1）的化合物及其酯，酰胺，酰胺/酯和盐，其中YCO是γ-Glu或β-asp; G *是苯基甘氨酸或甘氨酸; Z是CH 2，O或S; X为1-20 C的烃基; 可用于刺激骨髓分化，减轻化疗药物的骨髓破坏作用，增强化学治疗剂的毒性。

5. 发明授权

US4581224A Inhibition of undesired effect of platinum compounds 失效
标题翻译：抑制铂化合物的不良影响
公开(公告)号：US4581224A
公开(公告)日：1986-04-08
申请号：US568904
申请日：1984-01-05
申请人： Richard F. Borch
发明人： Richard F. Borch
IPC分类号： A61K31/095 , A61K31/28 , A61K31/325 , A61K31/27
CPC分类号： A61K31/325 , A61K31/095 , A61K31/28 , Y10S514/922 , Y10S514/974
摘要： Dithiocarbamic compounds, administered about 0.5 to about 6 hours after Pt compounds, have been found to counter the toxicity of the platinum in multi-cellular organisms (e.g. mammals). For example, neoplastic growths in mammals can be treated with cis-diamine or cis-diamine Pt(II) complexes with greatly lessened risk of nephrotoxicity, bone marrow toxicity, or damage to the digestive system of the mammal, provided the dithiocarbamic compound is timely (and preferably parenterally) administered. Particularly effective dithiocarbamic compounds are monomeric (e.g. ##STR1## where M is a pharmaceutically acceptable cation and R.sup.1 and R.sup.2 are lower aliphatic (or cycloaliphatic or heterocycloaliphatic groups) or, less preferably, dimeric, e.g. ##STR2## wherein R.sup.1 and R.sup.2 are as defined previously, and R.sup.3 and R.sup.4 are defined in the same manner as R.sup.1 and R.sup.2. These dithiocarbamic compounds do not significantly reduce the desired effect of the Pt(II) compounds (particularly when the dithiocarbamic compound is intravenously admininstered), despite their effectiveness in reducing harmful side effects.
摘要翻译：在Pt化合物后约0.5至约6小时施用的二硫代氨基甲酸酯化合物已经被发现抵抗铂在多细胞生物体（例如哺乳动物）中的毒性。例如，哺乳动物的肿瘤生长可用顺式 - 二胺或顺式 - 二胺Pt（II）配合物处理，如果二硫代氨基甲酸酯化合物是及时的，则可以大大降低肾毒性，骨髓毒性或对哺乳动物消化系统的损害（优选肠胃外）给药。特别有效的二硫代氨基甲酸酯化合物是单体的（例如，其中M是药学上可接受的阳离子，R 1和R 2是低级脂族（或脂环族或杂环脂肪族基团）或更不优选二聚体，例如其中R 1和R 2如所定义之前，R3和R4的定义与R1和R2相同，这些二硫代氨基甲酸酯化合物不会显着降低Pt（II）化合物的预期效果（特别是当二硫代氨基甲酸酯化合物静脉注射时），尽管它们有效地还原有害的副作用。

6. 发明授权

US4426372A Inhibition of undesired effects of platinum(II) compounds 失效
标题翻译：抑制铂（II）化合物的不期望的影响
公开(公告)号：US4426372A
公开(公告)日：1984-01-17
申请号：US176476
申请日：1980-08-08
申请人： Richard F. Borch
发明人： Richard F. Borch
IPC分类号： A61K31/095 , A61K31/28 , A61K31/325
CPC分类号： A61K31/28 , A61K31/095 , A61K31/325 , Y10S514/922
摘要： Dithiocarbamic compounds, administered about 0.5 to about 6 hours after Pt(II) compound, have been found to counter the toxicity of the platinum in multicellular organisms (e.g. mammals). For example, neoplastic growths in mammals can be treated with cis-diamine or cis-diammine Pt(II) complexes with greatly lessened risk of nephrotoxicity and damage to the digestive system of the mammal, provided the dithiocarbamic compound is timely (and preferably parenterally) administered. Particularly effective dithiocarbamic compounds are monomeric (e.g. ##STR1## where M.sup..sym. is a pharmaceutically acceptable cation and R.sup.1 and R.sup.2 are lower aliphatic or cycloaliphatic groups) or, less preferably, dimeric, e.g. ##STR2## wherein R.sup.1 and R.sup.2 are as defined previously, and R.sup.3 and R.sup.4 are defined in the same manner as R.sup.1 and R.sup.2. These dithiocarbamic compounds do not significantly reduce the desired effects of the Pt(II) compounds (particularly when the dithiocarbamic compound is intravenously administered), despite their effectiveness in reducing harmful side effects.
摘要翻译：在Pt（II）化合物后约0.5至约6小时施用的二硫代氨基甲酸酯化合物已被发现可抵抗铂在多细胞生物体（例如哺乳动物）中的毒性。例如，如果二硫代氨基甲酸酯化合物是及时的（优选肠胃外），哺乳动物的肿瘤生长可以用顺式二胺或顺式二氨基铂（II）配合物治疗，大大降低了肾毒性的风险并损害了哺乳动物的消化系统。管理。特别有效的二硫代氨基甲酸酯化合物是单体的（例如，其中M（+）是药学上可接受的阳离子，R 1和R 2是低级脂族基或脂环族基团），或者更优选二聚体。其中R1和R2如前所定义，R3和R4以与R1和R2相同的方式定义。这些二硫代氨基甲酸酯化合物不能显着降低Pt（II）化合物的所需效果（特别是当二硫代氨基甲酸酯化合物静脉内给药时），尽管它们有效地减少有害副作用。

7. 发明授权

US5233031A Phosphoramidate analogs of 2'-deoxyuridine 失效
标题翻译： 2'-脱氧酶的磷酸酯类似物
公开(公告)号：US5233031A
公开(公告)日：1993-08-03
申请号：US763936
申请日：1991-09-23
申请人： Richard F. Borch , Kristin M. Fries
发明人： Richard F. Borch , Kristin M. Fries
IPC分类号： A61K31/70 , A61K31/7042 , A61K31/7052 , A61K31/7064 , A61K31/7072 , A61P35/00 , C07H19/10
CPC分类号： C07H19/10
摘要： The present invention provides a series of cytotoxic phosphoramidate analogs of 5-fluoro-2'-deoxyuridine of the general formula (I): ##STR1## wherein R.sup.1 is H, F or (C.sub.1 -C.sub.4)alkyl; R.sup.2 is CH.sub.2 CH.sub.2 X wherein X is Cl, Br, I or p-toluenesulfonyl; R.sup.3 is (C.sub.1 -C.sub.4)alkyl or CH.sub.2 CH.sub.2 X wherein X is Cl, Br, I or p-toluenesulfonyl; or wherein R.sup.2 and R.sup.3, taken together with the N atom, can be a 5- or 6-membered heterocyclic ring which is aliphatic or aliphatic interrupted by a ring oxygen or a second ring nitrogen; R.sup.4 is H, one equivalent of a pharmaceutically-acceptable cation or (4,4,6-trimethyltetrahydro-1,3-oxazin-2-yl)ethyl, and the pharmaceutically-acceptable salts thereof.
摘要翻译：本发明提供了通式（I）的5-氟-2'-脱氧尿苷的一系列细胞毒性氨基磷酸酯类似物：其中R 1是H，F或（C 1 -C 4）烷基; R2是CH2CH2X，其中X是Cl，Br，I或对甲苯磺酰; R3是（C1-C4）烷基或CH2CH2X，其中X是Cl，Br，I或对甲苯磺酰基; 或其中R 2和R 3与N原子一起可以是被环氧或第二环氮中断的脂族或脂族的5或6元杂环; R4是H，1当量的药学上可接受的阳离子或（4,4,6-三甲基四氢-1,3-恶嗪-2-基）乙基及其药学上可接受的盐。

8. 发明授权

US5035878A Use of dithiocarbamates to counteract myelosuppression 失效
标题翻译：使用二硫代氨基甲酸盐来抵抗骨髓抑制
公开(公告)号：US5035878A
公开(公告)日：1991-07-30
申请号：US418549
申请日：1989-10-10
申请人： Richard F. Borch , Therese K. Schmalbach
发明人： Richard F. Borch , Therese K. Schmalbach
IPC分类号： A61K31/27 , A61K38/00 , C07K14/53 , C12N5/077
CPC分类号： C12N5/0669 , A61K31/27 , C07K14/53 , A61K38/00 , C12N2501/999 , Y10S514/823 , Y10S514/885 , Y10S514/922
摘要： Various types of biological treatments, including antineoplastic treatments with antineoplastic drugs, can result in damage to the blood-forming function of the bone marrow. This damage can be reversed, at least to some degree, with an effective amount (preferably an extremely low dose) of a pharmaceutically acceptable dithiocarbamic compound, including a compound of the formula R.sub.1 R.sub.2 NCSSM or R.sub.1 R.sub.2 NCSS-SCSNR.sup.3 R.sup.4, wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are the same or different aliphatic or cycloaliphatic or heterocycloaliphatic groups, unsubstituted or substituted by hydroxyl, or one of R.sup.1 and R.sup.2 and one of R.sup.3 and R.sup.4 can be H, or R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4, taken together with the N atom upon which the pair of R groups is substituted, can be a 5- or 6-member N-heterocyclic ring which is aliphatic or aliphatic interrupted by a ring oxygen or second ring nitrogen, and M is H or one equivalent of a pharmaceutically acceptable cation, in which case the rest of the molecule is negatively charged. The dosage in mammals can range from about 0.001 to 30 mg/kg of body weight. For larger mammals, including humans, a typical dosage unit is less than 10 mg/kg, e.g.
摘要翻译：各种类型的生物处理，包括抗肿瘤药物的抗肿瘤治疗可能会损害骨髓的血液形成功能。至少在某种程度上可以使用有效量（优选极低剂量）的药学上可接受的二硫代氨基甲酸酯化合物，包括式R1R2NCSSM或R1R2NCSS-SCSNR3R4的化合物，其中R 1，R 2，R 3和 R4是相同或不同的未取代或被羟基取代的脂族或脂环族或杂脂肪族基团，或R 1和R 2之一，R 3和R 4中的一个可以是H，或者R 1和R 2或R 3和R 4与N原子一起一对R基团被取代的基团可以是被环氧或第二环氮中断的脂族或脂族的5-或6-元N-杂环，M是H或一当量的药学上可接受的阳离子在这种情况下，分子的其余部分是带负电荷的。哺乳动物的剂量可以为约0.001至30mg / kg体重。对于较大的哺乳动物，包括人类，典型的剂量单位小于10mg / kg，例如 <3 mg / kg。剂量单位可以溶解在合适的药学上可接受的载体（例如水性介质）中，然后优选在施用可引起骨髓损伤的药物的8小时内静脉内施用。在本发明中特别优选的极低剂量不会引起任何显着的副作用。

9. 发明授权

US07304046B2 Phosphoramide compounds 失效
标题翻译：磷酰胺化合物
公开(公告)号：US07304046B2
公开(公告)日：2007-12-04
申请号：US10725191
申请日：2003-12-01
申请人： Richard F. Borch , Marcy Hernick , Carolee Flader
发明人： Richard F. Borch , Marcy Hernick , Carolee Flader
IPC分类号： A16K31/661 , C07F9/22
CPC分类号： C07F9/2416 , C07F9/5728
摘要： The invention provides a compound of formula I: wherein R1, Ra, Rb, Rc, and Rd have any of the values defined in the specification, as well as pharmaceutical compositions comprising such compounds or salts. The compounds are useful for treating cancer in animals.
摘要翻译：本发明提供式I化合物：

10. 发明授权

US07173020B2 Phosphoramidates and methods therefor 失效
标题翻译：磷酰胺化物及其方法
公开(公告)号：US07173020B2
公开(公告)日：2007-02-06
申请号：US11053024
申请日：2005-02-08
申请人： Richard F. Borch , Hugo Garrido-Hernandez , Sandra C. Tobias
发明人： Richard F. Borch , Hugo Garrido-Hernandez , Sandra C. Tobias
IPC分类号： A61K31/664
CPC分类号： C07H19/10 , C07F9/2458 , C07F9/26 , C07F9/65515 , C07F9/655345
摘要： Novel phosphoramidate derivatives of hydroxy functional or amino functional compounds, including amino acids, peptides, peptidomimetics and nucleotide analogs, are described. The compounds enable enhanced intracellular delivery of drugs as their corresponding phosphate esters or amides. Described phosphoramidate compounds exhibit antiproliferative activity. Pharmaceutical formulations are provided for treatment of cancers.
摘要翻译：描述了羟基官能或氨基官能化合物的新型氨基磷酸衍生物，包括氨基酸，肽，肽模拟物和核苷酸类似物。这些化合物能够增强药物的细胞内递送作为其相应的磷酸酯或酰胺。描述的氨基磷酸酯化合物表现出抗增殖活性。提供药物制剂用于治疗癌症。

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