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71. 发明申请

US20040024063A1 Fatty acid analogues for the treatment of cancer 失效
标题翻译：脂肪酸类似物用于治疗癌症
公开(公告)号：US20040024063A1
公开(公告)日：2004-02-05
申请号：US10312901
申请日：2003-01-02
发明人： Rolf Berge
IPC分类号： A61K031/20
CPC分类号： A61K31/19 , A61K31/20 , A61K31/22 , A61K31/23 , A61K31/255
摘要： The present invention relates to fatty acid analogues of general formula (I): R1-nullxi-CH2nullnnullCOOR2, wherein is: a C1-C24 alkene with one or more double bonds and/or with one or more triple bonds; and/or a C1-C24 alkyne, and/or a C1-C24 alkyl, or an alkyl substituted in one or several positions with one or more compounds selected from the group comprising fluoride, chloride, hydroxy, C1-C4 alkoxy, C1-C4 alkylthio, C2-C5 acyloxy or C1-C4 alkyl, and wherein R2 represents hydrogen or C1-C4 alkyl, and wherein is an integer from 1 to 12, and wherein i is an odd number and indicates the position relative to COOR2, and wherein Xi independent of each other are selected from the group comprising O, S, SO, SO2, Se and CH2, and with the proviso that at least one of the Xi is not CH2, which can be used for the treatment and/or prevention of primary and secondary metastatic neoplasms.
摘要翻译：本发明涉及通式（I）的脂肪酸类似物：R1- [xi-CH2] n-COOR2，其中：具有一个或多个双键和/或一个或多个三键的C 1 -C 24烯烃; 和/或C 1 -C 24炔基，和/或C 1 -C 24烷基，或在一个或多个位置被一个或多个选自以下的化合物取代的烷基：氟，氯，羟基，C 1 -C 4烷氧基， C4烷硫基，C2-C5酰氧基或C1-C4烷基，其中R2表示氢或C1-C4烷基，其中为1〜12的整数，其中i为奇数，表示相对于COOR2的位置，其中彼此独立的X选自O，S，SO，SO 2，Se和CH 2的基团，并且条件是至少一个X 1不是CH 2，其可以用于治疗和/或预防的原发性和继发性转移性肿瘤。

72. 发明申请

US20030165486A1 Compositions and methods for the induction of retinal detachments 有权
标题翻译：用于诱导视网膜脱离的组合物和方法
公开(公告)号：US20030165486A1
公开(公告)日：2003-09-04
申请号：US10160135
申请日：2002-05-31
发明人： Hampar L. Karageozian
IPC分类号： A61K038/47 , A61K031/08 , A61K035/78 , A61K031/20
CPC分类号： A61K45/06 , A61K31/045 , A61K31/08 , A61K31/19 , A61K31/191 , A61K31/198 , A61K31/20 , A61K31/23 , A61K31/231 , A61K31/341 , A61K31/765 , A61K31/77
摘要： A method comprising administering by ocular route a dose of a glycol ether effective to induce retinal detachment.
摘要翻译：一种方法，其包括通过眼睛途径施用有效诱导视网膜脱离的剂量的二醇醚。

73. 发明申请

US20030045543A1 Systems and methods for treating a mucosal surface 失效
公开(公告)号：US20030045543A1
公开(公告)日：2003-03-06
申请号：US10238662
申请日：2002-09-10
申请人： 3M Innovative Properties Company
发明人： John C. Hedenstrom , Michael J. Jozwiakowski , Mark Martinez , Kenneth R. Phares , Kenneth Trofatter JR.
IPC分类号： A61K031/4745 , A61K031/20
CPC分类号： C07D471/04 , A61K9/0014 , A61K9/0034 , A61K31/437 , A61K31/4745 , A61K31/4748 , A61K47/10 , A61K47/12 , A61M31/00 , A61M2210/1475
摘要： A system for treating a condition associated with a mucosal surface, the system comprising an immune response modifier (IRM) compound chosen from imidazoquinoline amines, imidazopyridine amines, 6,7-fused cycloalkylimidazopyridine amines, imidazonaphthyridine amines, oxazoloquinoline amines, thiazoloquinoline amines, 1,2-bridged imidazoquinoline amines, and pharmaceutically acceptable salts thereof and an applicator device for applying the IRM compound to the mucosal surface. This system of IRM compounds and applicator may be used to treat conditions associated with mucosal surfaces such as cervical dysphasia and cervical intraepithelial neoplasia.

74. 发明申请

US20030045524A1 Alpha-2-adrenergic agonist/fatty acid compositions 审中-公开
标题翻译： α-2-肾上腺素能激动剂/脂肪酸组合物
公开(公告)号：US20030045524A1
公开(公告)日：2003-03-06
申请号：US10136263
申请日：2002-05-01
发明人： David F. Woodward , Gyorgy Ambrus
IPC分类号： A61K031/498 , A61K031/20
CPC分类号： A61K31/20 , A61K31/00 , A61K31/19 , A61K31/495 , A61K31/557 , A61K2300/00
摘要： Compositions comprising an alpha-2-adrenergic agonist component and a fatty acid component, that enhances the pharmacokinetic disposition of the therapeutic component, are disclosed. The fatty acid component may include linolenic acid and/or other fatty acids. In a one embodiment, the alpha-2-adrenergic agonist component and the fatty acid component form a complex.
摘要翻译：公开了包含α-2-肾上腺素能激动剂组分和脂肪酸组分的组合物，其增强了治疗组分的药代动力学配置。脂肪酸组分可以包括亚麻酸和/或其它脂肪酸。在一个实施方案中，α-2-肾上腺素能激动剂组分和脂肪酸组分形成复合物。

75. 发明申请

US20020198259A1 Novel fatty acid analogues for the treatment and prevention of diseases caused by the pathological proliferation of smooth muscle cells 失效
标题翻译：新型脂肪酸类似物用于治疗和预防由平滑肌细胞病理增生引起的疾病
公开(公告)号：US20020198259A1
公开(公告)日：2002-12-26
申请号：US10151203
申请日：2002-05-17
发明人： Rolf Berge
IPC分类号： A61K031/22 , A61K031/23 , A61K031/20
CPC分类号： A61K31/28 , A23L33/115 , A23L33/12 , A61K31/19 , A61K31/20 , A61K31/215 , A61K31/22 , A61K31/23 , A61K31/255 , Y10S514/866
摘要： The present invention relates to novel fatty acid analogues of the general formula (I): CH3nullnullCH2nullmnullnullxinullCH2nullnnullCOOR, wherein n is an integer from 1 to 12, and wherein m is an integer from 0 to 23, and wherein i is an odd number which indicates the position relative to COOR, and wherein Xi independent of each other are selected from the group comprising O, S, SO, SO2, Se and CH2, and wherein R represents hydrogen or C1-C4 alkl, with the proviso that at least one of the Xi is not CH2, or a salt, prodrug or complex thereof, for the preparation of a pharmaceutical composition for the treatment and/or prevention of primary and/or secondary stenosis. Further the present invention relates to the use of said compounds for the prevention and/or treatment of a disease caused by procedural vascular trauma and/or pathological proliferation of smooth muscle cells, and/or an increased level of plasma homocysteine.
摘要翻译：本发明涉及通式（I）的新型脂肪酸类似物：CH 3 - [CH 2] m - [xi-CH 2] n -COOR，其中n为1至12的整数，并且其中m为 0至23，并且其中i是表示相对于COOR的位置的奇数，并且其中彼此独立的Xi选自包含O，S，SO，SO 2，Se和CH 2的基团，并且其中R表示氢或 C1-C4烷基，条件是至少一个X 1不是CH 2，或其盐，前药或复合物，用于制备用于治疗和/或预防原发性和/或继发性狭窄的药物组合物。此外，本发明涉及所述化合物用于预防和/或治疗由平滑肌细胞的程序性血管创伤和/或病理性增殖引起的疾病和/或血浆高半胱氨酸水平升高的用途。

76. 发明申请

US20020143052A1 Histone deacetylase inhibitors 有权
标题翻译：组蛋白脱乙酰酶抑制剂
公开(公告)号：US20020143052A1
公开(公告)日：2002-10-03
申请号：US09812945
申请日：2001-03-27
发明人： Hsuan-Yin Lan-Hargest , Robert J. Kaufman , Norbert L. Wiech
IPC分类号： A61K031/20 , A61K031/16 , A61K031/34
CPC分类号： A61K31/16 , C07C57/42 , C07C57/60 , C07C259/06 , C07D307/54
摘要： Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group or a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.
摘要翻译：组蛋白脱乙酰酶是在活性位点具有锌的金属酶。具有锌结合部分的化合物，例如异羟肟酸基或羧酸基可以抑制组蛋白脱乙酰酶。组蛋白脱乙酰酶抑制可抑制基因表达，包括与肿瘤抑制相关的基因的表达。因此，组蛋白脱乙酰酶的抑制可以提供用于治疗癌症，血液学疾病，例如血红蛋白病和遗传相关代谢紊乱（例如囊性纤维化和肾上腺脑白质营养不良）的替代途径。

77. 发明申请

US20020128326A1 TOPICAL IMMUNOMODULATING COMPOSITIONS FOR TREATMENT OF AIDS, HEPATITIS B&C, OTHER INFECTIOUS DISEASES, AND CANCER 失效
标题翻译：用于治疗艾滋病，乙型肝炎，其他感染性疾病和癌症的局部免疫调节组合物
公开(公告)号：US20020128326A1
公开(公告)日：2002-09-12
申请号：US09459935
申请日：1999-12-13
发明人： LEONARD L. KAPLAN , WILLIAM R. LEVIS
IPC分类号： A61K031/47 , A61K031/20 , A61K031/015
CPC分类号： A61K9/0014 , A61K31/015 , A61K31/20 , A61K31/47 , A61K45/06 , A61K47/14 , A61K47/26 , A61K2300/00
摘要： Topical drug compositions, containing contact sensitizing agents as the active components of the subject patent compositions, can provide a pharmacological action that induces a delayed hypersensitization reaction resulting in stimulation of cell mediated immunity when applied to the skin. The preferred composition contains, but is not limited to, Diphenylcyclpropenone as a preferred embodiment of the class of contact sensitizing drugs applied to the skin in an optimally prepared pharmaceutical formulation with controlled absorption properties to reach the peripheral circulation resulting in increases in CD4null helper T cells of benefit to immunocompromised patients.
摘要翻译：含有作为主题专利组合物的活性成分的接触敏化剂的局部药物组合物可以提供诱导延缓的超敏化反应的药理作用，导致当施用于皮肤时刺激细胞介导的免疫。优选的组合物包含但不限于二苯基环丙烯酮，作为在最佳制备的药物制剂中施用于皮肤的接触敏化药物类别的优选实施方案，具有受控的吸收性能以达到外周循环，导致CD4 +辅助T细胞增加对免疫功能低下的患者有益。

78. 发明申请

US20020120006A1 Retinoic acid receptor antagonists as promoters of angiogenesis 失效
标题翻译：视黄酸受体拮抗剂作为血管发生的启动子
公开(公告)号：US20020120006A1
公开(公告)日：2002-08-29
申请号：US09951306
申请日：2001-09-13
发明人： Violetta Iotzova , Peter Reczek
IPC分类号： A61K031/215 , A61K031/20
CPC分类号： A61K31/19 , A61K31/203
摘要： Methods and compositions for treating various disorders by administering a therapeutically effective amount of a retinoic acid receptor antagonist alone or in combination or in conjunction with other therapeutic agents to promote angiogenesis are provided. Also provided are methods for obtaining additional retinoic acid receptor antagonists for use as therapeutic agents to promote angiogenesis.
摘要翻译：提供了通过单独施用治疗有效量的视黄酸受体拮抗剂或与其它治疗剂组合或联合以促进血管生成来治疗各种疾病的方法和组合物。还提供了获得用作促进血管生成的治疗剂的另外的视黄酸受体拮抗剂的方法。

79. 发明申请

US20020082297A1 Composition comprising a carrier and a purified mycobacterial lipid cell-wall component and its use in the prevention, treatment and diagnosis of disease 审中-公开
标题翻译：包含载体和纯化的分枝杆菌脂质细胞壁组分的组合物及其在预防，治疗和诊断疾病中的用途
公开(公告)号：US20020082297A1
公开(公告)日：2002-06-27
申请号：US09847365
申请日：2001-05-02
申请人： ADCOCK INGRAM LIMITED
发明人： Jan Adrianus Verschoor , Anne Lenaerts , Elzbieta Johannsen
IPC分类号： A61K031/23 , A61K031/20 , C07C051/43
CPC分类号： A61K39/04 , A61K2039/544 , A61K2039/6043 , G01N33/5308 , G01N33/5695 , Y10S514/924
摘要： A composition including a purified lipid cell-wall component or analog or derivative thereof and a suitable pharmaceutical carrier, medium, excipient or adjuvant is described. The composition is useful in prophylactic and therapeutic methods of treating a microbial infection in a subject, typically a mycobacterial infection such as tuberculosis, and immune disorders, inflammatory conditions and allergies in a subject, typically autoimmune diseases. It is also useful in diagnostic methods. The purified lipid cell-wall component is typically a purified mycolic acid or a mixture of purified mycolic acids form a bacterium which produces mycolic acids. The bacterium if from Mycobacterium, Corynbacterium, Nocardia or Rhodococcus.
摘要翻译：描述了包含纯化的脂质细胞壁组分或其类似物或衍生物和合适的药物载体，培养基，赋形剂或佐剂的组合物。该组合物可用于治疗受试者的微生物感染的预防和治疗方法，通常是分枝杆菌感染如结核病，以及受试者中的免疫疾病，炎性病症和过敏症，通常为自身免疫性疾病。它也可用于诊断方法。纯化的脂质细胞壁组分通常是纯化的霉菌酸或纯化的霉菌酸的混合物，形成产生霉菌酸的细菌。来自分枝杆菌，棒杆菌，诺卡氏菌或红球菌的细菌。

80. 发明申请

US20020077358A1 Use of hydroperoxyeicosatetraenoic acid derivatives following refractive surgery 审中-公开
$Use of hydroperoxyeicosatetraenoic acid derivatives following refractive surgery$
标题翻译：屈光手术后使用氢过氧二十碳四烯酸衍生物
公开(公告)号：US20020077358A1
公开(公告)日：2002-06-20
申请号：US09965506
申请日：2001-09-27
申请人： Alcon Universal Ltd.
发明人： John M. Yanni , Daniel A. Gamache , Steven T. Miller
IPC分类号： A61K031/22 , A61K031/20 , A61K031/16
CPC分类号： A61K31/22 , A61K31/131 , A61K31/16 , A61K31/20 , A61K31/202 , A61K31/557
摘要： The use of HETE derivatives to treat dry eye conditions associated with refractive surgery is disclosed.
摘要翻译：公开了使用HETE衍生物来治疗与屈光手术相关的干眼症状。

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