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1. 发明授权

US06803379B2 PHARMACOLOGICAL AGENTS AND METHODS OF TREATMENT THAT INACTIVATE PATHOGENIC PROKARYOTIC AND EUKARYOTIC CELLS AND VIRUSES BY ATTACKING HIGHLY CONSERVED DOMAINS IN STRUCTURAL METALLOPROTEIN AND METALLOENZYME TARGETS 失效
标题翻译：药物代谢物和通过攻击结构性金属蛋白酶和金属碘化物目标中的高保守域来灭活病原性原核生物和原核细胞和病毒的治疗方法
公开(公告)号：US06803379B2
公开(公告)日：2004-10-12
申请号：US10161981
申请日：2002-06-04
申请人： Jose A. Fernandez-Pol , Sebastian Fernandez-Pol
发明人： Jose A. Fernandez-Pol , Sebastian Fernandez-Pol
IPC分类号： A61K3141
CPC分类号： A61K45/06 , A61K31/341 , A61K31/345 , A61K31/381 , Y02A50/411 , A61K2300/00
摘要： The invention relates to the treatment of viral, bacterial, parasitic, proliferative diseases, neurodegenerative diseases, inflammatory diseases, immunological diseases, transplanted organ rejection, and diseases produced by intoxication with heavy metals. The invention relates to the use of specific metal chelating agents including, furoic acid, 2-thiophenecarboxylic acid and their derivatives, analogs and structurally related chemicals as pharmacological agents that can be used effectively to disrupt and inactivate specific transition metal ion containing zinc finger structural motifs in metalloproteins and specific transition metal ion containing catalytic sites in metalloproteinases, which in turn, inactivate the pathogenic virus, pathogenic prokaryotic or eukaryotic cells which produces disease conditions. The preparations can be administered topically or for systemic use. The preparations are novel wide-spectrum antibiotics which have antiviral, antiproliferative, antineoplastic, antiangiogenic, antibacterial, antiparasitic, antiinfective, and anti-inflammatory effects and can be used in the treatment and prevention of diseases such as AIDS, cancers, untoward angiogenesis, pulmonary anthrax, malaria, inflammatory responses, Alzheimer's disease and other diseases.
摘要翻译：本发明涉及病毒，细菌，寄生虫，增殖性疾病，神经退行性疾病，炎性疾病，免疫性疾病，移植器官排斥反应以及由重金属中毒产生的疾病的治疗。本发明涉及特定金属螯合剂的使用，包括糠酸，2-噻吩羧酸及其衍生物，类似物和结构相关的化学物质作为可有效地用于破坏和灭活含特定过渡金属离子的锌指结构基序的药理学在金属蛋白质和金属蛋白酶中含有催化位点的特定过渡金属离子中，这反过来会使致病病毒，致病原核或真核细胞产生疾病状况失活。制剂可以局部给药或全身用药。该制剂是具有抗病毒，抗增殖，抗肿瘤，抗血管生成，抗菌，抗寄生虫，抗感染和抗炎作用的新型广谱抗生素，可用于治疗和预防艾滋病，癌症，不良血管生成，肺部疾病炭疽，疟疾，炎症反应，阿尔茨海默病和其他疾病。

2. 发明授权

US06734201B1 8-Azaprostaglandin carbonate and thiocarbonate analogs as therapeutic agents 失效
标题翻译： 8-Azaprostaglandin碳酸酯和硫代碳酸酯类似物作为治疗剂
公开(公告)号：US06734201B1
公开(公告)日：2004-05-11
申请号：US10453818
申请日：2003-06-02
申请人： David W. Old , Thang D. Dinh , Robert M. Burk
发明人： David W. Old , Thang D. Dinh , Robert M. Burk
IPC分类号： A61K3141
CPC分类号： C07D207/26 , C07D403/06 , C07F9/572
摘要： The present invention provides a compound represented by the general formula I; wherein A, Ar, X, Z, n, x, y, R and R3 are as defined in the specification.
摘要翻译：本发明提供由通式I表示的化合物，其中A，Ar，X，Z，n，x，y，R和R 3如说明书中所定义。

3. 发明授权

US06727266B2 Substituted tryptophan derivatives 失效
标题翻译：取代色氨酸衍生物
公开(公告)号：US06727266B2
公开(公告)日：2004-04-27
申请号：US10169836
申请日：2002-07-10
申请人： Fumihiko Watanabe
发明人： Fumihiko Watanabe
IPC分类号： A61K3141
CPC分类号： C07D403/12 , C07D409/12 , C07D413/12
摘要： A compound of the formula (I): wherein: R1 is represented by the formula: wherein R4, R5, R6, R7 and R8 are monovalent radicals such as: hydrogen, halogen, optionally substituted lower alkyl, lower alkyloxy, lower alkylthio, optionally substituted amino, nitro; non-aromatic heterocyclic group, and the like with certain provisos; Y is —OH or —NHOH; R2 is hydrogen, optionally substituted lower alkyl, or optionally substituted aralkyl; R3 is halogen, hydroxy, lower alkyloxy, or lower alkylthio; (b) n is an integer from 1 to 3; its optically active substance, its prodrug, its pharmaceutically acceptable salt, and its solvate.
摘要翻译：式（I）的化合物：其中：R 1由下式表示：其中R 4，R 5，R 6，R 7和R 8是单价基团，如：氢，卤素，任选取代的低级烷基，低级烷氧基，低级烷硫基，任选取代的氨基，硝基; 非芳族杂环基等具有某些条件; Y为-OH或-NHOH; R 2为氢，任选取代的低级烷基或任选取代的芳烷基; R 3为卤素，羟基，低级烷氧基，或低级烷硫基;（b）n为1至3的整数;其光学活性物质，其前药，其药学上可接受的盐及其溶剂合物。

4. 发明授权

US06455557B1 Method of reducing somnolence in patients treated with tizanidine 有权
标题翻译：减少使用替扎尼定治疗患者嗜睡的方法
公开(公告)号：US06455557B1
公开(公告)日：2002-09-24
申请号：US09994837
申请日：2001-11-28
申请人： Cara A. Pellegrini , Paul Stark
发明人： Cara A. Pellegrini , Paul Stark
IPC分类号： A61K3141
CPC分类号： A61K31/433 , A61K9/0002 , A61K9/1676 , A61K9/48 , A61K9/4808 , A61K9/50 , A61K31/41 , A61K31/415
摘要： An article and method for reducing somnolence in a patient receiving tizanidine therapy. Tizanidine may be administered in the form of an immediate release multiparticulate composition at or around the time food is consumed. The composition may be packaged in a container for distribution.
摘要翻译：一种减轻接受替扎尼定治疗的患者嗜睡的文章和方法。替扎尼定可以在食物消耗的时间或周围以立即释放多颗粒组合物的形式施用。组合物可以包装在容器中用于分配。

5. 发明授权

US06426359B1 Prevention and treatment of skeletal disorder with EP2 receptor subtype selective prostaglandin E2 agonists 失效
标题翻译：用EP2受体亚型选择性前列腺素E2激动剂预防和治疗骨骼疾病
公开(公告)号：US06426359B1
公开(公告)日：2002-07-30
申请号：US09331078
申请日：1999-06-11
申请人： Kimberly O. Cameron , Hua Z. Ke , Bruce A. Lefker , Robert L Rosati , David D. Thompson
发明人： Kimberly O. Cameron , Hua Z. Ke , Bruce A. Lefker , Robert L Rosati , David D. Thompson
IPC分类号： A61K3141
CPC分类号： A61K31/195 , A61K31/00 , A61K31/18 , A61K31/192 , A61K31/197 , A61K31/20 , A61K31/381 , A61K31/41
摘要： This invention relates to the use of EP2 receptor subtype selective prostaglandin E2 agonists to augment bone mass including the prevention and treatment of skeletal disorders in mammals, including humans.
摘要翻译：本发明涉及EP2受体亚型选择性前列腺素E2激动剂用于增加骨量的用途，包括预防和治疗哺乳动物（包括人）中的骨骼疾病。

6. 发明授权

US06420399B1 Topical ophthalmic mast cell stabilizers for treating allergic eye disease 有权
标题翻译：用于治疗过敏性眼病的局部眼用肥大细胞稳定剂
公开(公告)号：US06420399B1
公开(公告)日：2002-07-16
申请号：US09527401
申请日：2000-03-16
申请人： Gustav Graff , John M. Yanni
发明人： Gustav Graff , John M. Yanni
IPC分类号： A61K3141
CPC分类号： A61K31/55 , A61K31/41 , Y10S514/912
摘要： Topical ophthalmic anti-allergy drugs are identified by the extent of their interaction with a phospholipid model membrane. Disclosed are topically administrable ophthalmic formulations containing amphipathic anti-allergy compounds at concentrations such that the drugs have Surface Activity Ratings from about 2-11.
摘要翻译：局部眼用抗过敏药物通过与磷脂模型膜相互作用的程度来鉴定。公开了含有两性抗过敏化合物的局部给药的眼用制剂，其浓度使得药物具有约2-11的表面活性等级。

7. 发明授权

US06407129B1 Azole compounds, their production and their use 失效
标题翻译：唑类化合物，其生产及其用途
公开(公告)号：US06407129B1
公开(公告)日：2002-06-18
申请号：US09381479
申请日：1999-09-20
申请人： Katsumi Itoh , Tomoyuki Kitazaki , Kenji Okonogi
发明人： Katsumi Itoh , Tomoyuki Kitazaki , Kenji Okonogi
IPC分类号： A61K3141
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08
摘要： A quaternized nitrogen-containing imidazol-1-yl or 1,2,4-triazol-1-yl compound wherein one of the nitrogen atoms constituting an azole ring is quaternized with a substituent capable of being eliminated in vivo and the substituent can be eliminated in vivo to be converted into an antifungal azole compound, has an improved solubility in water, can advantageously be applied to injection, has an improved internal absorption and can be expected to have a good effect for the treatment or prevention of disease.
摘要翻译：构成唑环的氮原子之一的季铵化的含氮咪唑-1-基或1,2,4-三唑-1-基化合物被能够在体内消除的取代基季铵化，并且可以消除取代基在体内被转化为抗真菌唑化合物，在水中的溶解度提高，可有利地应用于注射，具有改善的内部吸收，并且可以预期对于治疗或预防疾病具有良好的效果。

8. 发明授权

US06380222B2 Use of an H+, K+-atpase inhibitor in the treatment of nasal polyps 失效
标题翻译：使用H +，K + -ATPase抑制剂治疗鼻息肉
公开(公告)号：US06380222B2
公开(公告)日：2002-04-30
申请号：US09833699
申请日：2001-04-13
申请人： Per Lindberg , Joan Piñas-Massó , Jordi Serra-Carreras , Jan Trofast
发明人： Per Lindberg , Joan Piñas-Massó , Jordi Serra-Carreras , Jan Trofast
IPC分类号： A61K3141
CPC分类号： A61K31/435 , A61K9/0014 , A61K31/4184 , A61K31/437 , A61K31/4439 , A61K31/56 , A61K31/573 , A61K31/58 , A61K45/06 , A61K31/57 , A61K2300/00
摘要： The invention provides a method for the treatment of polyposis which comprises treating a subject suffering from polyposis with an H+,K+-ATPase inhibitor and, optionally, a glucocorticoid. The invention also relates to a pharmaceutical formulation for simultaneous, separate or sequential administration in the treatment of Widal's Syndrome and in the treatment of asthma.
摘要翻译：本发明提供一种治疗息肉病的方法，其包括用H +，K + -ATP酶抑制剂和任选的糖皮质激素治疗患有息肉病的受试者。本发明还涉及用于在治疗Widal氏综合征和哮喘治疗中同时，分别或连续给药的药物制剂。

9. 发明授权

US06348481B2 Pharmaceutical composition for angiotensin II-mediated diseases 失效
公开(公告)号：US06348481B2
公开(公告)日：2002-02-19
申请号：US09758355
申请日：2001-01-12
申请人： Yoshiyuki Inada , Keiji Kubo
发明人： Yoshiyuki Inada , Keiji Kubo
IPC分类号： A61K3141
CPC分类号： A61K45/06 , A61K31/495 , A61K31/54 , A61K31/415 , A61K2300/00
摘要： This invention relates to a pharmaceutical composition for angiotensin II-mediated diseases, which comprises a compound having angiotensin II antagonistic activity of the formula wherein R1 is H or an optionally substituted hydrocarbon residue; R2 is an optionally esterified carboxyl group; R3 is a group capable of forming an anion or a group convertible thereinto; X is a covalent bond between the 2 phenyl rings or a spacer having a chain length of 1 to 2 atoms as the linear moiety between the adjoining phenylene group and phenyl group; n is 1 or 2; the ring A is a benzene ring having 1 or 2 optional substituents in addition to R2; and Y is a bond, —O—, —S(O)m— (wherein m is 0, 1 or 2) or —N(R4)— (wherein R4 is H or an optionally substituted alkyl group), or a pharmaceutically acceptable salt thereof in combination with a compound having diuretic activity or a compound having calcium antagonistic activity.

10. 发明授权

US06281233B1 Method of treating gastrointestinal motility disorders 失效
公开(公告)号：US06281233B1
公开(公告)日：2001-08-28
申请号：US08485418
申请日：1995-06-07
申请人： Beverley Greenwood
发明人： Beverley Greenwood
IPC分类号： A61K3141
CPC分类号： C07D451/04 , C07D453/02 , C07D471/08 , C07D487/08 , Y10S514/867
摘要： The present invention relates to a novel method for treating a mammal suffering from gastrointestinal motility disorders.

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